Microwave-assisted synthesis of pomalidomide building blocks for rapid PROTAC and molecular glue development

Diaaeldin I. Abdallah, Johan Israelian, Lina S. Hasan, Naman H. Patel, Jeffrey W. Keillor, Timothy B. Wright, Bilal Saqib, Elvin D. de Araujo and Patrick T. Gunning

Chem. Commun., 2025, 61, 4670
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An effective strategy for balancing energy and sensitivity: design, synthesis, and properties of chimeric energetic molecules

Yujia Shan, Shi Huang, Tianyu Jiang, Ye Cao, Jinxin Wang, Yuteng Cao and Wenquan Zhang

J. Mater. Chem. A, 2025, 13, 1164
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Chemical tools for probing histidine modifications

Nurgül Bilgin, Jordi C. J. Hintzen and Jasmin Mecinović

Chem. Commun., 2025, 61, 3805
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Design and synthesis of nucleic acid nano-environment interactome-targeting small molecule PROTACs and their anticancer activity

Sadiya Tanga, Arkadeep Karmakar, Arpita Hota, Paramita Banerjee and Basudeb Maji

Nanoscale, 2024, 16, 12502
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Cu-catalysed three-component C–H trifluoroalkylation of glycine derivatives: access to diverse CF3-containing amino acids

Yadong Li, Dengfu Lu and Yuefa Gong

Org. Chem. Front., 2023, 10, 2301
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Molecule engineering strategy of toll-like receptor 7/8 agonists designed for potentiating immune stimuli activation

Liuwei Gu, Xiaojie Kong, Mengyan Li, Rui Chen, Ke Xu, Guo Li, Yulin Qin and Li Wu

Chem. Commun., 2024, 60, 5474
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Recent advances in focal adhesion kinase (FAK)-targeting antitumor agents

Si-Kai Zhu, Qi Wu, Guang-Xin Liu, An-Qi Geng and Ping-An Wang

RSC Adv., 2025, 15, 20957
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Design, synthesis and evaluation of pyrrolobenzodiazepine (PBD)-based PROTAC conjugates for the selective degradation of the NF-κB RelA/p65 subunit

Peiqin Jin, Md. Mahbub Hasan, Andrea G. S. Pepper, Simon Mitchell, Khondaker Miraz Rahman and Chris Pepper

RSC Med. Chem., 2025
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Proximity-inducing modalities: the past, present, and future

Sameek Singh, Wenzhi Tian, Zachary C. Severance, Santosh K. Chaudhary, Viktoriya Anokhina, Basudeb Mondal, Rajaiah Pergu, Prashant Singh, Uttam Dhawa, Santanu Singha and Amit Choudhary

Chem. Soc. Rev., 2023, 52, 5485
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Discovery of a selective TC-PTP degrader for cancer immunotherapy

Jinmin Miao, Jiajun Dong, Yiming Miao, Yunpeng Bai, Zihan Qu, Brenson A. Jassim, Bo Huang, Quyen Nguyen, Yuan Ma, Allison A. Murray, Jinyue Li, Philip S. Low and Zhong-Yin Zhang

Chem. Sci., 2023, 14, 12606
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PROTAC chemical probes for histone deacetylase enzymes

Urvashi Patel, Joshua P. Smalley and James T. Hodgkinson

RSC Chem. Biol., 2023, 4, 623
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Hydrophobic CPP/HDO conjugates: a new frontier in oligonucleotide-warheaded PROTAC delivery

Miyako Naganuma, Nobumichi Ohoka, Motoharu Hirano, Daishi Watanabe, Genichiro Tsuji, Takao Inoue and Yosuke Demizu

RSC Med. Chem., 2024, 15, 3695
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Topical BET PROTACs for locally restricted protein degradation in the lung

Martin Hemmerling, Jianming Liu, Antonio Piras, Rikard Pehrson, Ulf Hedström, Carlo Cassani, Beatrice Ranieri, Karolina Kwapień, Karin Ribbing, Cecilia Forss, Oliwia Slettengren, Frederik Eisele, Mei Ding, Pia Hansson, Anna Novén, Markus Nordberg, Hyunsoo Park, Annica Jarke, Lisa-Catherine Rosenbaum, Jesper Malmberg, Annika Borde, Lassina Badolo, Madeleine Engsevi, Johan Jirholt, Perla Breccia, Stefan Schiesser, Lena Ripa and Werngard Czechtizky

RSC Med. Chem., 2025
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Property-based optimisation of PROTACs

James S. Scott, Iacovos N. Michaelides and Markus Schade

RSC Med. Chem., 2025, 16, 449
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Use of ionic liquids in amidation reactions for proteolysis targeting chimera synthesis

Michela Eleuteri, Jenny Desantis, Gabriele Cruciani, Raimondo Germani and Laura Goracci

Org. Biomol. Chem., 2024, 22, 3477
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PROTACs bearing piperazine-containing linkers: what effect on their protonation state?

Jenny Desantis, Andrea Mammoli, Michela Eleuteri, Alice Coletti, Federico Croci, Antonio Macchiarulo and Laura Goracci

RSC Adv., 2022, 12, 21968
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Polymer-engineered PROTAC nanovehicles amplify synergistic effects with temozolomide by BRD4 degradation

Yun Guo, Haoyu You, Yiyang Li, Zheng Zhou, Zonghua Tian, Chen Jiang and Tao Sun

Biomater. Sci., 2025
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Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance

Rouming Peng, Xin Liu, Chun-Chi Chen, Rey-Ting Guo and Jian Min

RSC Med. Chem., 2025, 16, 1023
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An ultrasonically sensitive small-molecule chimera for sono-controllable proteolysis

Bin Zhang, Siyi Wang, Chen Li, Sisi Zhou, Yan Zhang, Guifang Xu and Jinbo Li

Chem. Commun., 2025, 61, 12550
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A platinated prodrug leveraging PROTAC technology for targeted protein degradation and enhanced antitumor efficacy

Jiaqian Xu, Shu Chen, Ka-Yan Ng, Xianfeng Chen, Wai Chung Fu and Guangyu Zhu

Inorg. Chem. Front., 2025, 12, 3981
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Nano-PROTACs: state of the art and perspectives

Jie Zhong, Ruiqi Zhao, Yuji Wang, Yu-xiong Su and Xinmiao Lan

Nanoscale, 2024, 16, 4378
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Methods to characterize and discover molecular degraders in cells

Zhi Lin and Christina M. Woo

Chem. Soc. Rev., 2022, 51, 7115
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Chemistries of bifunctional PROTAC degraders

Chaoguo Cao, Ming He, Liguo Wang, Yuna He and Yu Rao

Chem. Soc. Rev., 2022, 51, 7066
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Innovative, combinatorial and high-throughput approaches to degrader synthesis

Rebecca Stevens, James D. F. Thompson, Julie C. L. Fournier, Glenn A. Burley, David J. Battersby and Afjal H. Miah

Chem. Soc. Rev., 2024, 53, 4838
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Protacs in cancer therapy: mechanisms, design, clinical trials, and future directions

Akash Vikal, Rashmi Maurya, Brij Bihari Patel, Rajeev Sharma, Preeti Patel, Umesh K. Patil and Balak Das Kurmi

Drug Deliv. and Transl. Res., 2025, 15, 1801
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Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation

Yasheng Zhu, Xiuquan Ye, Yuxing Wu, Hao Shen, Zeyu Cai, Fei Xia, Wenjian Min, Yi Hou, Liping Wang, Xiao Wang, Yibei Xiao and Peng Yang

J. Med. Chem., 2024, 67, 7283
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Development of Proteasome Inhibitors for Cancer Therapy

Xu Chen, Xuan Wu, Linyan Li and Xiaoming Zhu

IJDDP, 2024, 100004
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Discovery of a first-in-class PROTAC degrader of histone lysine demethylase KDM4

Danni Rao, Yiting Wang, Xiaolong Yang, Zhiwen Chen, Feifei Wu, Ran Ren, Yaoliang Sun, Yuanhui Lai, Lijie Peng, Lei Yu, Zhang Zhang and Shilin Xu

European Journal of Medicinal Chemistry, 2025, 288, 117410
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A Physiologically Responsive Nanocomposite Hydrogel for Treatment of Head and Neck Squamous Cell Carcinoma via Proteolysis‐Targeting Chimeras Enhanced Immunotherapy

Yaping Wu, Xiaowei Chang, Guizhu Yang, Li Chen, Qi Wu, Jiamin Gao, Ran Tian, Wenyun Mu, John Justin Gooding, Xin Chen and Shuyang Sun

Advanced Materials, 2023, 35
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BET degraders reveal BRD4 disruption of 7SK and P-TEFb is critical for effective reactivation of latent HIV in CD4+ T-cells

Anne-Marie W. Turner, Frances M. Bashore, Shane D. Falcinelli, Joshua A. Fox, Alana L. Keller, Anthony D. Fenton, Renee F. Geyer, Brigitte Allard, Jennifer L. Kirchherr, Nancie M. Archin, Lindsey I. James, David M. Margolis and Viviana Simon

J Virol, 2025, 99
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Recent Advances of Degradation Technologies Based on PROTAC Mechanism

Mingchao Xiao, Jiaojiao Zhao, Qiang Wang, Jia Liu and Leina Ma

Biomolecules, 2022, 12, 1257
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Chem-map profiles drug binding to chromatin in cells

Zutao Yu, Jochen Spiegel, Larry Melidis, Winnie W. I. Hui, Xiaoyun Zhang, Antanas Radzevičius and Shankar Balasubramanian

Nat Biotechnol, 2023, 41, 1265
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SE(3)-equivariant ternary complex prediction towards target protein degradation

Fanglei Xue, Meihan Zhang, Shuqi Li, Xinyu Gao, James A. Wohlschlegel, Wenbing Huang, Yi Yang and Weixian Deng

Nat Commun, 2025, 16
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Discovery of Novel Proteolysis-Targeting Chimera Molecules as Degraders of Programmed Cell Death-Ligand 1 for Breast Cancer Therapy

Hongjia Zhang, Yan Zhang, Zhanzhan Feng, Ming Shuai, Xinyu Ma, Shirui Wang, Su Yu, Rui Deng, Dan Luo, Jianyou Shi, Chunlan Pu and Rui Li

J. Med. Chem., 2024, 67, 10589
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Ligand discovery by activity-based protein profiling

Micah J. Niphakis and Benjamin F. Cravatt

Cell Chemical Biology, 2024, 31, 1636
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Advancements in Proteolysis Targeting Chimeras for Targeted Therapeutic Strategies in Alzheimer’s Disease

Qiuzhi Zhou, Weixia Wang and Chunchu Deng

Mol Neurobiol, 2025, 62, 9686
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Photodynamic enhancement of PROTAC prodrug activation in hypoxic tumors

Zhongliang Fu, Chunrong Yang, Yuchen Yang, Meichen Pan, Hongwei Hou and Jinghong Li

Acta Pharmaceutica Sinica B, 2025
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A new tau dephosphorylation-targeting chimera for the treatment of tauopathies

Jing-fen Su, Yue Xiao, Lin-yu Wei, Hui-yang Lei, Fei Sun, Wei-xia Wang, Shi-hong Li, Xiao-chuan Wang, Jie Zheng and Jian-zhi Wang

Acta Pharmacol Sin, 2024, 45, 2267
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Discovery of a New and Selective HPK1 PROTAC for Enhancing Tumor Immunotherapy through Eliminating GLK Degradation

Mingfei Wu, Xinfei Mao, Yiquan Wu, Wentao Wang, Yuyuan Jin, Hengyuan Yu, Liuzhi Hu, Zheyuan Shen, Liteng Shen, Shenxin Zeng, Tengfei Xu, Yong Chen, Bo Zhang, Nengming Lin, Jinxin Che, Wenhai Huang and Xiaowu Dong

J. Med. Chem., 2025, 68, 10800
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Dissecting and targeting noncanonical functions of EZH2 in multiple myeloma via an EZH2 degrader

Xufen Yu, Jun Wang, Weida Gong, Anqi Ma, Yudao Shen, Chengwei Zhang, Xijuan Liu, Ling Cai, Jing Liu, Gang Greg Wang and Jian Jin

Oncogene, 2023, 42, 994
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Discovery of a Novel CRBN-Recruiting cGAS PROTAC Degrader for the Treatment of Ulcerative Colitis

Peng He, Chengming Wen, Xinyu Zhang and Hang Yin

J. Med. Chem., 2025, 68, 5551
DOI: 10.1021/acs.jmedchem.4c02774

N-Boc-α-diazo glutarimide as efficient reagent for assembling N-heterocycle-glutarimide diads via Rh(II)-catalyzed N–H insertion reaction

Grigory Kantin, Pavel Golubev, Alexander Sapegin, Alexander Bunev and Dmitry Dar’in

Beilstein J. Org. Chem., 2023, 19, 1841
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Revolutionizing Drug Targeting Strategies: Integrating Artificial Intelligence and Structure-Based Methods in PROTAC Development

Danishuddin, Mohammad Sarwar Jamal, Kyoung-Seob Song, Keun-Woo Lee, Jong-Joo Kim and Yeong-Min Park

Pharmaceuticals, 2023, 16, 1649
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Quantum Mechanics-Based Ranking of Predicted Proteolysis Targeting Chimeras-Mediated Ternary Complexes

Stefania Monteleone, Inaki Morao, Dmitri G. Fedorov and Tahsin F. Kellici

ACS Med. Chem. Lett., 2025, 16, 420
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MMP-2-triggered, mitochondria-targeted PROTAC-PDT therapy of breast cancer and brain metastases inhibition

Fan Tong, Yufan Wang, Yanyan Xu, Yang Zhou, Siqin He, Yufan Du, Wenqin Yang, Ting Lei, Yujun Song, Tao Gong and Huile Gao

Nat Commun, 2024, 15
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Macrocyclic Peptide-Based Dual-Sensor Platform for Linkage-Specific Visualization of Ubiquitin Chain Assembling in Live Cells

Han Gao, Zhirong He, Jian Chen, Huixia Feng, Rui Zhao and Yanyan Huang

Anal. Chem., 2025, 97, 2351
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Glucose Transporter-Targeting Chimeras Enabling Tumor-Selective Degradation of Secreted and Membrane Proteins

Chengyu Yun, Na Li, Yishu Zhang, Tong Fang, Jing Ma, Zhenting Zheng, Subing Zhou and Xiaoqing Cai

ACS Chem. Biol., 2024, 19, 2254
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Discovery of a Potent, selective and orally bioavailable CDK9 degrader for targeting transcription regulation in Triple-Negative breast cancer

Hui-Jun Nie, Ben-Fu Li, Jingya Sun, Yali Yuan, Zhi-Gao Zhang, Hao Hu, Wen-Jing Wang, Ziqiang Chen, Simei Wang, Wensi Huang, Xingxing Diao, Jinghua Yu, Ruimin Huang and Xiao-Hua Chen

Bioorganic Chemistry, 2024, 153, 107876
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Current strategies for improving limitations of proteolysis targeting chimeras

Chunlan Pu, Shirui Wang, Lei Liu, Zhonghui Feng, Hongjia Zhang, Qianyuan Gong, Yueshan Sun, Yuanbiao Guo and Rui Li

Chinese Chemical Letters, 2023, 34, 107927
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Liver-targeting chimeras as a potential modality for the treatment of liver diseases

Chuanjie Chen, Yongzhang Pan, Xiaoyu Yang, Huiqin Li, Xinhui Cai, Shengyuan He, Qiong Wang, Yiwen Yang, Runzi Zheng, Huiwen Li, Shengjie Yuan, Xin Dong, Priyadarshani Nadeeshika Samarawickrama, Meiting Zi, Yonghan He and Xuan Zhang

Journal of Controlled Release, 2024, 374, 627
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A BPTF-specific PROTAC degrader enhances NK cell-based cancer immunotherapy

Yunjia Li, Lin Bai, Hao Liang, Peidong Yan, Hao Chen, Zhuoxian Cao, Yiqing Shen, Zhongyv Wang, Mei Huang, Bin He, Quan Hao, Yide Mei, Haiming Wei, Chen Ding, Jing Jin and Yi Wang

Molecular Therapy, 2025, 33, 1566
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Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives

Jiarui Hu, Dan Zhang, Keyue Tian, Changyu Ren, Heng Li, Congcong Lin, Xiaoli Huang, Jie Liu, Wuyu Mao and Jifa Zhang

European Journal of Medicinal Chemistry, 2023, 256, 115475
DOI: 10.1016/j.ejmech.2023.115475

Nanoenabled Strategies Enhancing PROTACs for Cancer Therapy

Rui Li, Shuhao Zhang, Yunxue Xu, Renfa Liu and Zhifei Dai

Bioconjugate Chem., 2025, 36, 1582
DOI: 10.1021/acs.bioconjchem.5c00305

Design, synthesis and biological evaluation of novel TMPRSS2-PROTACs with florosubstituted 4-guanidino-N-phenylbenzamide derivative ligands

Hao Yang, Haoran Xu, Xinxin Lin, Zengxuan Cai, Yong Xia, Yu Wang, Zejie Chen, Koutian Zhang, Yanling Wu, Jianwei Wang, Annoor Awadasseid and Wen Zhang

Bioorganic & Medicinal Chemistry, 2024, 116, 117982
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Protein-Based Degraders: From Chemical Biology Tools to Neo-Therapeutics

Lisha Ou, Mekedlawit T. Setegne, Jeandele Elliot, Fangfang Shen and Laura M. K. Dassama

Chem. Rev., 2025, 125, 2120
DOI: 10.1021/acs.chemrev.4c00595

Annual review of PROTAC degraders as anticancer agents in 2022

Xiao Wang, Zhao-Long Qin, Na Li, Mei-Qi Jia, Qiu-Ge Liu, Yi-Ru Bai, Jian Song, Shuo Yuan and Sai-Yang Zhang

European Journal of Medicinal Chemistry, 2024, 267, 116166
DOI: 10.1016/j.ejmech.2024.116166

Design, Synthesis, and Evaluation of BCL‐2 Targeting PROTACs

Aleša Bricelj, Yuen Lam Dora Ng, Martina Gobec, Robert Kuchta, Wanyi Hu, Špela Javornik, Miha Rožič, Michael Gütschow, Guangrong Zheng, Jan Krönke, Christian Steinebach and Izidor Sosič

Chemistry A European J, 2024, 30
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Targeting RNA‐binding proteins with small molecules: Perspectives, pitfalls and bifunctional molecules

Qingxin Li and Congbao Kang

FEBS Letters, 2023, 597, 2031
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Revolutionizing lung cancer treatment: Introducing PROTAC therapy as a novel paradigm in targeted therapeutics

Atharva Mahajan, Gauri Panzade, Tiyasa Bhuniya, Purbasha Das, Bidyabati Bhattacharjee, Sagnik Das, Ankita Chowdhury, Kashmira Chakraborty, Sudeepta Guha, Anushka Samant, Anuvab Dey and Subhrojyoti Ghosh

Current Problems in Cancer, 2025, 54, 101172
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Toosendanin: upgrade of an old agent in cancer treatment

Shuwei LI, Qingyi XIONG, Yiwen SHEN, Jiayi LIN, Lijun ZHANG, Ye WU, Jinmei JIN and Xin LUAN

Chinese Journal of Natural Medicines, 2024, 22, 887
DOI: 10.1016/S1875-5364(24)60693-X

Self-assembly strategies of organic small-molecule photosensitizers for photodynamic therapy

Xiaohui Xiong, Jingyuan Liu, Lei Wu, Shuangyu Xiong, Wen Jiang and Peng Wang

Coordination Chemistry Reviews, 2024, 510, 215863
DOI: 10.1016/j.ccr.2024.215863

PROTACs in platelets: emerging antithrombotic strategies and future perspectives

Justin S. Trory, Jordan Vautrinot, Carl J. May and Ingeborg Hers

Current Opinion in Hematology, 2025, 32, 34
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Split‐Cas9‐based targeted gene editing and nanobody‐mediated proteolysis‐targeting chimeras optogenetically coordinated regulation of Survivin to control the fate of cancer cells

Changping Deng, Shihui Li, Yuping Liu, Wen Bao, Chengnan Xu, Wenyun Zheng, Meiyan Wang and Xingyuan Ma

Clinical & Translational Med, 2023, 13
DOI: 10.1002/ctm2.1382

Conjugation with glucagon like peptide-1 enables targeted protein degradation

Liquan Zhu, Yiyu Zhou, Bei Zhang, Yin Luo, Chen Fang, Xiaoqiao Yan, Yefeng Cai, Linye Jiang and Jingyan Ge

Bioorganic Chemistry, 2023, 141, 106908
DOI: 10.1016/j.bioorg.2023.106908

Design, synthesis, and biological evaluation of RIPK1-targeting PROTACs

Hefeng Zhang, Shuonan Zhang, Tianchen Wang, Yaohan Lan, Yang Dai, Xia Peng, Yuxiang An, Yi Xue, Jing Ai and Wenhu Duan

Mol Divers, 2025
DOI: 10.1007/s11030-025-11166-x

ClpP-based MtPTAC technology enables targeted degradation of inner mitochondrial membrane proteins

Yuxin Yao, Dachi Wang, Haoyu Gong, Ruibin Jiang, Yang Liu, Yijun Liu, Xin Lai, Zhaoyang Xu, Wei Zhou, Haorong Li and Xiaohong Fang

Bioorganic & Medicinal Chemistry, 2025, 130, 118350
DOI: 10.1016/j.bmc.2025.118350

A Structural Investigation of the Interaction between a GC-376-Based Peptidomimetic PROTAC and Its Precursor with the Viral Main Protease of Coxsackievirus B3

Alessia De Santis, Deborah Grifagni, Andrea Orsetti, Elena Lenci, Antonio Rosato, Mariapina D’Onofrio, Andrea Trabocchi, Simone Ciofi-Baffoni, Francesca Cantini and Vito Calderone

Biomolecules, 2024, 14, 1260
DOI: 10.3390/biom14101260

Fragment-Based Interrogation of the 14–3–3/TAZ Protein–Protein Interaction

Blaž Andlovic, Dario Valenti, Federica Centorrino, Francesca Picarazzi, Stanimira Hristeva, Malgorzata Hiltmann, Alexander Wolf, François-Xavier Cantrelle, Mattia Mori, Isabelle Landrieu, Laura M. Levy, Bert Klebl, Dimitrios Tzalis, Thorsten Genski, Jan Eickhoff and Christian Ottmann

Biochemistry, 2024, 63, 2196
DOI: 10.1021/acs.biochem.4c00248

Aurora kinases, emerging critical targets for cancer treatment and related new therapeutic strategies

Sua Chung, Ella Sperier, Kevin Graciano, Xiaoping Hu, Hua Guo and Jia Xu

Bioorganic Chemistry, 2025, 163, 108633
DOI: 10.1016/j.bioorg.2025.108633

DCAF16‐Based Covalent Molecular Glues for Targeted Protein Degradation of Histone Deacetylases

Tao Sun, Shiyang Zhai, Stephan Lepper, Beate König, Mateo Malenica, Irina Honin and Finn K. Hansen

Archiv der Pharmazie, 2025, 358
DOI: 10.1002/ardp.70045

Advances in Ubiquitination and Proteostasis in Retinal Degeneration

Jia Wei, Xiaona Chen, Yingyue Xiong and Yali Gao

Front. Biosci. (Landmark Ed), 2024, 29
DOI: 10.31083/j.fbl2907260

Modulating the phosphorylation status of target proteins through bifunctional molecules

Qindi He, Zhijie Wang, Rongrong Wang, Tao Lu, Yadong Chen and Shuai Lu

Drug Discovery Today, 2025, 30, 104307
DOI: 10.1016/j.drudis.2025.104307

Development of DNA Aptamer-Based PROTACs That Degrade the Estrogen Receptor

Haruna Tsujimura, Miyako Naganuma, Nobumichi Ohoka, Takao Inoue, Mikihiko Naito, Genichiro Tsuji and Yosuke Demizu

ACS Med. Chem. Lett., 2023, 14, 827
DOI: 10.1021/acsmedchemlett.3c00126

Targeted degradation of specific TEAD paralogs by small molecule degraders

Hui Chen, Artem Gridnev, Netanya Schlamowitz, Wanyi Hu, Kuntala Dey, Guangrong Zheng and Jyoti R. Misra

Heliyon, 2024, 10, e37829
DOI: 10.1016/j.heliyon.2024.e37829

DNA Nanotechnology for Application in Targeted Protein Degradation

Yang Xiao, Xinyi Guo, Weiwei Zhang, Lequn Ma and Kewei Ren

ACS Biomater. Sci. Eng., 2024, 10, 6814
DOI: 10.1021/acsbiomaterials.4c01351

New insights into the dule roles CDK12 in human cancers: Mechanisms and interventions for cancer therapy

Wei Dai, Dong Xie, Hao Huang, Jingxuan Li, Caiyao Guo, Fuqiang Cao, Luo Yang, Chengyong Zhong and Shenglan Liu

Journal of Pharmaceutical Analysis, 2025, 15, 101173
DOI: 10.1016/j.jpha.2024.101173

Discovering a potent and orally available imidazopyridine derivative as a BRD4 inhibitor: Enhancing antiproliferative activity against melanoma cells by mitigating P-gp substrate recognition

Yuhei Horai, Naoki Suda, Shinsuke Uchihashi, Mayako Katakuse, Tomomi Shigeno, Takashige Hirano, Junichi Takahara, Tomoyuki Fujita, Yohei Mukoyama and Yuji Haga

Bioorganic & Medicinal Chemistry, 2025, 129, 118337
DOI: 10.1016/j.bmc.2025.118337

Proteolysis‐Targeting Chimera (PROTAC): A Revolutionary Tool for Chemical Biology Research

Meichen Pan, Zhongliang Fu, Hongwei Hou, Chunrong Yang and Jinghong Li

Small Methods, 2025, 9
DOI: 10.1002/smtd.202500402

Delivering on Cell‐Selective Protein Degradation Using Chemically Tailored PROTACs

Rui Yao, Tianli Luo and Ming Wang

ChemBioChem, 2023, 24
DOI: 10.1002/cbic.202300413

LSD1 in drug discovery: From biological function to clinical application

Hui‐Min Liu, Ying Zhou, He‐Xiang Chen, Jiang‐Wan Wu, Shi‐Kun Ji, Liang Shen, Shao‐Peng Wang, Hong‐Min Liu, Ying Liu, Xing‐Jie Dai and Yi‐Chao Zheng

Medicinal Research Reviews, 2024, 44, 833
DOI: 10.1002/med.22000

Advancing brain tumor therapy: unveiling the potential of PROTACs for targeted protein degradation

Saooda Ibrahim, Muhammad Umer Khan, Saadia Noreen, Safia Firdous, Iqra Khurram, Raima Rehman, Muhammad Arshad Javed and Qurban Ali

Cytotechnology, 2025, 77
DOI: 10.1007/s10616-025-00716-8

X‐Ray‐Induced Drug Release for Cancer Therapy

Hui Liu, Jun Zhao, Yufei Xue, Jiaxin Zhang, Hua Bai, Sijun Pan, Bo Peng, Lin Li and Nicolas H. Voelcker

Angewandte Chemie, 2023, 135
DOI: 10.1002/ange.202306100

Advancing target validation with PROTAC technology

M. Leora Spitz, Aseel Kashkush and Raphael I. Benhamou

Expert Opinion on Drug Discovery, 2025, 20, 551
DOI: 10.1080/17460441.2025.2490248

Structural optimization and characterization of highly potent and selective STAT3 inhibitors for the treatment of triple negative breast cancer

Wangrui Jin, Yuzhu Zhang, Baozhen Wang, Zhaoyong Kang, Huachao Li, Jingfeng Song, Yihua Chen, Hai Xiong and Jing Chen

European Journal of Medicinal Chemistry, 2025, 287, 117332
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DNA nanoflower Oligo-PROTAC for targeted degradation of FUS to treat neurodegenerative diseases

Ruixin Ge, Miao Chen, Sijin Wu, Sirui Huang, Ping Zhou, Minghui Cao, Fan Zhang, Jinzhi Zang, Yigao Zhu, Jingrui Li, Guilin Ni, Zhihao Yang, Qingchao Li, Wei Pan, Liang Zhang, Min Liu, Chenghao Xuan, Haiyang Yu, Jun Zhou and Songbo Xie

Nat Commun, 2025, 16
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Recent Development of CDK2 Inhibitors as Anticancer Drugs: An Update (2015–2023)

Yumei Jin, Hao Lu, Hu Ge, Xuben Hou and Hao Fang

Pharmaceutical Fronts, 2024, 06, e195
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Programmable Circular Multivalent Nanobody‐Targeting Chimeras (mNbTACs) for Multireceptor‐Mediated Protein Degradation and Targeted Drug Delivery

Shiqi Jiang, Xinru Lv, Zhenlin Ouyang, Hongli Chi, Yuchen Zeng, Yani Wang, Jiaxuan He, Jinling Chen, Jingyi Chen, Keli An, Ming Cheng, Yurong Wen, Juan Li and Penghui Zhang

Angewandte Chemie, 2024, 136
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Unmasking the tumourigenic role of SIN1/MAPKAP1 in the mTOR complex 2

Emilien Ezine, Céleste Lebbe and Nicolas Dumaz

Clinical & Translational Med, 2023, 13
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Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer

Shilong Ying, Hongli Chi, Xiaoqiu Wu, Pingping Zeng, Jinling Chen, Ting Fu, Weitao Fu, Penghui Zhang and Weihong Tan

J. Med. Chem., 2024, 67, 17053
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A region-confined PROTAC nanoplatform for spatiotemporally tunable protein degradation and enhanced cancer therapy

Jing Gao, Xingyu Jiang, Shumin Lei, Wenhao Cheng, Yi Lai, Min Li, Lei Yang, Peifeng Liu, Xiao-hua Chen, Min Huang, Haijun Yu, Huixiong Xu and Zhiai Xu

Nat Commun, 2024, 15
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Navigating PROTACs in Cancer Therapy: Advancements, Challenges, and Future Horizons

Saooda Ibrahim, Muhammad Umer Khan, Iqra Khurram, Raima Rehman, Abdur Rauf, Zubair Ahmad, Abdullah S. M. Aljohani, Waleed Al Abdulmonem and Mohammed Mansour Quradha

Food Science & Nutrition, 2025, 13
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Perspective Strategies for Interventions in Parkinsonism: Remedying the Neglected Role of TPPP

Judit Oláh, Vic Norris, Attila Lehotzky and Judit Ovádi

Cells, 2024, 13, 338
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Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders

Felix Feller, Irina Honin, Martina Miranda, Heiko Weber, Svenja Henze, Maria Hanl and Finn K. Hansen

J. Med. Chem., 2025, 68, 1824
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Cereblon neo-substrate binding mimics the recognition of the cyclic imide degron

Christopher Heim, Anna-Katharina Spring, Sören Kirchgäßner, Dirk Schwarzer and Marcus D. Hartmann

Biochemical and Biophysical Research Communications, 2023, 646, 30
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Overcoming cancer therapy resistance: From drug innovation to therapeutics

Jin-Rui Wei, Meng-Yi Lu, Tian-Hua Wei, Joshua S. Fleishman, Hui Yu, Xiao-Li Chen, Xiang-Tu Kong, Shan-Liang Sun, Nian-Guang Li, Ye Yang and Hai-Wen Ni

Drug Resistance Updates, 2025, 81, 101229
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Cell Membrane as A Promising Therapeutic Target: From Materials Design to Biomedical Applications

Xiaofeng Wu, Jing‐Jing Hu and Juyoung Yoon

Angewandte Chemie, 2024, 136
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An instructive attempt on developing aptamer-constructed PROTAC for breast cancer treatment

Yuzhu Zhang, Dazhao Mi and Yihua Chen

Molecular Therapy - Nucleic Acids, 2022, 30, 351
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Advancing PROTAC Characterization: Structural Insights through Adducts and Multimodal Tandem-MS Strategies

Mohammed Rahman, Bryan Marzullo, Stephen W. Holman, Mark Barrow, Andrew D. Ray and Peter B. O’Connor

J. Am. Soc. Mass Spectrom., 2024, 35, 285
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Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders

Jian Chen, Wentao Zhu, Wenqian Zhang, Yichen Tong, Fang Xu and Jiyan Pang

ACS Med. Chem. Lett., 2024, 15, 659
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Targeted degradation of α-synuclein by arginine-based PROTACs

Linjing Shen, Jianchao Zhang, Zhaoran Wang, Yaxuan Liu, Shengjin Cui and Hai Rao

Journal of Biological Chemistry, 2025, 301, 110449
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MOF-based nanoparticles for tumor-targeted protein degradation and photodynamic therapy induce enhanced anti-tumor immunity

Huanhuan Zhu, Fei Gao, Yuan Li, Min Jiang, Yue Zhang, Chen Kan, Lin Han, Shaobo Xue, Kesheng Wang, Qiangyuan Fan, Honggang Hu, Fenyong Sun and Zunzhen Ming

Nano Today, 2024, 56, 102308
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PROteolysis‐Targeting Chimeras (PROTACs) in leukemia: overview and future perspectives

André T. S. Vicente and Jorge A. R. Salvador

MedComm, 2024, 5
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Nano Proteolysis Targeting Chimeras (PROTACs) with Anti‐Hook Effect for Tumor Therapy

Ni‐Yuan Zhang, Da‐Yong Hou, Xing‐Jie Hu, Jian‐Xiao Liang, Man‐Di Wang, Zhang‐Zhi Song, Li Yi, Zhi‐Jia Wang, Hong‐Wei An, Wanhai Xu and Hao Wang

Angew Chem Int Ed, 2023, 62
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Covalent Recruitment of NEDD4 for Targeted Protein Degradation: Rational Design of Small Molecular Degraders

Xiaoqiang He, Shihan Zeng, Yalei Wen, Tao Yang, Chaoming Huang, Yifang Li, Zhang Zhang, Ke Ding, Tongzheng Liu, Yi Tan and Zhengqiu Li

J. Am. Chem. Soc., 2025, 147, 21512
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Dual-PROTACs based on natural product derivative potassium dehydrographolide succinate: design, synthesis, and antitumor activity of a novel EGFR degrader

Ruling Shi, Peixi Zhang, Ming Chen, Weiming Lu, Meng Xu, Huagong Zeng, Jie He, Yan Wang, Yirong Lin and Jieqing Liu

Med Chem Res, 2025, 34, 1695
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Sono‐Responsive Hydrogel for Fractionated PROTAC Release to Alleviate Resistance and Immunosuppression Induced by Multi‐Course Postoperative Radiotherapy

Haiyang Wang, Yixuan Hou, Taian Lin, Ihsan Ullah, Qing Xu, Ye Liu, Taosha Jin, Yangning Zhang and Youyong Yuan

Adv Funct Materials, 2025
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Discovery of a brain-permeable bromodomain and extra terminal domain (BET) inhibitor with selectivity for BD1 for the treatment of multiple sclerosis

Xuetao Chen, Tingting Wu, Zhiyan Du, Wenjing Kang, Rujun Xu, Fanying Meng, Chihong Liu, Yali Chen, Qichao Bao, Jingkang Shen, Qidong You, Danyan Cao, Zhengyu Jiang and Xiaoke Guo

European Journal of Medicinal Chemistry, 2024, 265, 116080
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Ligation to Scavenging Strategy Enables On-Demand Termination of Targeted Protein Degradation

Yuhui Jin, Jing Fan, Ruyan Wang, Xuanyu Wang, Ning Li, Qidong You and Zhengyu Jiang

J. Am. Chem. Soc., 2023, 145, 7218
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Proteolysis targeting chimera of BI-2536 induces potent dual degradation of PLK1 and BET proteins

Shiwei Song, Wanrong Yang and Wanyi Tai

Bioorganic & Medicinal Chemistry, 2025, 120, 118087
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Classifying covalent protein binders by their targeted binding site

Walaa A. Bedewy, John W. Mulawka and Marc J. Adler

Bioorganic & Medicinal Chemistry Letters, 2025, 117, 130067
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Recent advances in targeted protein degraders as potential therapeutic agents

Na Yang, Bo Kong, Zhaohong Zhu, Fei Huang, Liliang Zhang, Tao Lu, Yadong Chen, Yanmin Zhang and Yulei Jiang

Mol Divers, 2024, 28, 309
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The Peptide PROTAC Modality: A New Strategy for Drug Discovery

Youmin Zhu, Yu Dai and Yuncai Tian

MedComm, 2025, 6
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Current Status of Oligonucleotide-Based Protein Degraders

Po-Chang Shih, Miyako Naganuma, Yosuke Demizu and Mikihiko Naito

Pharmaceutics, 2023, 15, 765
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Self-Assembled Nano-PROTAC Enables Near-Infrared Photodynamic Proteolysis for Cancer Therapy

Weishan Wang, Chenghong Zhu, Bin Zhang, Yi Feng, Yan Zhang and Jinbo Li

J. Am. Chem. Soc., 2023, 145, 16642
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Incorporating a β-hairpin sequence motif to increase intracellular stability of a peptide-based PROTAC

Hannah C. Hymel, Jeffery C. Anderson, Dong Liu, Ted J. Gauthier and Adam T. Melvin

Biochemical Engineering Journal, 2023, 199, 109063
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MicroRNA‐Triggered Programmable DNA‐Encoded Pre‐PROTACs for Cell‐Selective and Controlled Protein Degradation

Jiayin Zhan, Xiang Li, Zhe Feng, Zheng Liu, Zhiyuan Feng, Jun‐Jie Zhu and Jingjing Zhang

Angewandte Chemie, 2025, 137
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The application of targeted protein degradation technologies to G protein‐coupled receptors

Alastair C. Keen, Manuela Jörg and Michelle L. Halls

British J Pharmacology, 2024, 181, 2351
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Discovery of Potent Dual PROTAC Degraders Targeting BET-Kinase To Overcome FLT3 Inhibitor Resistance

Qiuping Xiang, Yujie Sun, Hui Hua, Mengdie Hu, Xiaomei Li, Manyu Guo, Le Niu, Zhang Zhang, Ting Cai and Dongsheng Zhu

J. Med. Chem., 2025, 68, 17303
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Small-molecule-based targeted therapy in liver cancer

Yue Ming, Yanqiu Gong, Xuewen Fu, Xinyu Ouyang, Yong Peng and Wenchen Pu

Molecular Therapy, 2024, 32, 3260
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Targeted delivery of PROTAC-based prodrug activated by bond-cleavage bioorthogonal chemistry for microneedle-assisted cancer therapy

Jing Huang, Zhuo Yao, Bowen Li and Yuan Ping

Journal of Controlled Release, 2023, 361, 270
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Discovery of a first-in-class degrader for the protein arginine methyltransferase 6 (PRMT6)

Hongling Yang, Qiangsheng Zhang, Shuyan Zhou, Zuli Hu, Qing Tang, Zulong Li, Qiang Feng and Luoting Yu

Bioorganic Chemistry, 2024, 148, 107439
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Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer

Si Ha, Chenxuan Ji, Jiaqi Yang, Maoxu Xiao, Ziyi Xu, Wei-Wei Pan, Hua Xiang and Guoshun Luo

European Journal of Medicinal Chemistry, 2025, 282, 117079
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Optimization of the PROTAC linker region of the proteasome substrate receptor hRpn13 rationalized by structural modeling with molecular dynamics

Xiuxiu Lu, Venkata R. Sabbasani, Bakar Hassan, Rolf E. Swenson and Kylie J. Walters

Journal of Biological Chemistry, 2025, 301, 108520
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A Medicinal Chemistry Perspective on Protein Tyrosine Phosphatase Nonreceptor Type 2 in Tumor Immunology

Qi Huang, Linghao Hu, Haowen Chen, Bingjie Yang, Xun Sun and Mingliang Wang

J. Med. Chem., 2025, 68, 3995
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Advances in designing ternary complexes: Integrating in-silico and biochemical methods for PROTAC optimisation in target protein degradation

Shareef Shaik, Prasanna Kumar Reddy Gayam, Manish Chaudhary, Gurvinder Singh and Aravinda Pai

Bioorganic Chemistry, 2024, 153, 107868
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A breast cancer targeted photodynamic degrader to activate immunotherapy through EGFR degradation mediated PD-L1 downregulation

Yuxuan Wei, Zuxiao Chen, Chuyu Huang, Hong Cheng, Xiaofeng Jiang and Shiying Li

Chemical Engineering Journal, 2024, 488, 150822
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Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

Yerim Jin and Yeongju Lee

ChemMedChem, 2024, 19
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Discovery of Highly Potent Nicotinamide Phosphoribosyltransferase Degraders for Efficient Treatment of Ovarian Cancer

Kaijian Bi, Junfei Cheng, Shipeng He, Yuxin Fang, Min Huang, Chunquan Sheng and Guoqiang Dong

J. Med. Chem., 2023, 66, 1048
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Facilitating the development of molecular glues: Opportunities from serendipity and rational design

Weiqing Jiang, Yunhan Jiang, Youfu Luo, Wenliang Qiao and Tao Yang

European Journal of Medicinal Chemistry, 2024, 263, 115950
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Exploring the Mechanisms, Biomarkers, and Therapeutic Targets of TRIM Family in Gastrointestinal Cancer

Chunyan Weng, Rijuan Jin, Xiaoliang Jin, Zimei Yang, Chenghai He, Qiuhua Zhang, Jingli Xu and Bin Lv

DDDT, 2024, Volume 18, 5615
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MicroRNA‐Triggered Programmable DNA‐Encoded Pre‐PROTACs for Cell‐Selective and Controlled Protein Degradation

Jiayin Zhan, Xiang Li, Zhe Feng, Zheng Liu, Zhiyuan Feng, Jun‐Jie Zhu and Jingjing Zhang

Angew Chem Int Ed, 2025, 64
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Journey of PROTAC: From Bench to Clinical Trial and Beyond

Kyli Berkley, Julian Zalejski, Nidhi Sharma and Ashutosh Sharma

Biochemistry, 2025, 64, 563
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Targeted Protein Acetylation Through Chemically Induced Proximity

Wesley W. Wang, Soumya Jyoti Singha Roy and Christopher G. Parker

Acc. Chem. Res., 2025
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Checkpoint Nano‐PROTACs for Activatable Cancer Photo‐Immunotherapy

Chi Zhang, Mengke Xu, Shasha He, Jingsheng Huang, Cheng Xu and Kanyi Pu

Advanced Materials, 2023, 35
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Expanding the horizons of targeted protein degradation: A non-small molecule perspective

Xiaowei Huang, Fengbo Wu, Jing Ye, Lian Wang, Xiaoyun Wang, Xiang Li and Gu He

Acta Pharmaceutica Sinica B, 2024, 14, 2402
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Decoding estrogen receptor and GPER biology: structural insights and therapeutic advances in ERα−positive breast cancer

Taniya Saha and Kiven Erique Lukong

Front. Oncol., 2025, 15
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Formation of C(sp2)–C(sp3) Bonds Instead of Amide C–N Bonds from Carboxylic Acid and Amine Substrate Pools by Decarbonylative Cross-Electrophile Coupling

Jiang Wang, Lauren E. Ehehalt, Zhidao Huang, Omar M. Beleh, Ilia A. Guzei and Daniel J. Weix

J. Am. Chem. Soc., 2023, 145, 9951
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BRD4-targeted photodegradation nanoplatform for light activatable melanoma therapy

Shiman Lu, Zhaoqing Shi, Chendi Ding, Wenyan Wang, Weilang Zhang, Li Huang, Jiachan Lin, Xinpei Wang, Ran Luo, Xiaowei Zeng, Wenhu Zhou, Hongzhong Chen, Qiangsong Wang and Lin Mei

Biomaterials, 2025, 317, 123101
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ROTACs leverage signaling-incompetent R-spondin for targeted protein degradation

Rui Sun, Zibo Meng, Hyeyoon Lee, Rienk Offringa and Christof Niehrs

Cell Chemical Biology, 2023, 30, 739
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Discovery of a Highly Potent PROTAC Degrader of p300/CBP Proteins for the Treatment of Enzalutamide-Resistant Prostate Cancer

Mengjun Ma, Mengyao Li, Chengwei Zhang, Zixuan Yang, Xiaoyu Chen, Penghui Lu, Shuangshuang Nie, Siqi Zhang, Shumin Ma and Chong Qin

J. Med. Chem., 2024, 67, 17290
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Modulating Phosphorylation by Proximity-Inducing Modalities for Cancer Therapy

Qiuyue Zhang, Jia Yu, Qidong You and Lei Wang

J. Med. Chem., 2024, 67, 21695
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Photo-regulated PROTACs: A novel tool for temporal control of targeted protein degradation

Hanqiao Xu, Nobumichi Ohoka, Takao Inoue, Hidetomo Yokoo and Yosuke Demizu

Bioorganic & Medicinal Chemistry Letters, 2024, 107, 129778
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Small-Molecule PROTACs for Cancer Immunotherapy

Zefan Liu, Yajun Zhang, Yucheng Xiang and Xin Kang

Molecules, 2022, 27, 5439
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Activatable PROTAC nanoassembly for photodynamic PTP1B proteolysis enhances glioblastoma immunotherapy

Yeongji Jang, Jiwoong Choi, Byeongmin Park, Jung Yeon Park, Jae-Hyeon Lee, Jagyeong Goo, Dongwon Shin, Sun Hwa Kim, Yongju Kim, Hyun Kyu Song, Jooho Park, Kwangmeyung Kim, Yoosoo Yang and Man Kyu Shim

Acta Pharmaceutica Sinica B, 2025
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Targeted Strategies for Degradation of Key Transmembrane Proteins in Cancer

Vehary Sakanyan, Nina Iradyan and Rodolphe Alves de Sousa

BioTech, 2023, 12, 57
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Ferroptosis Nanomedicine: Clinical Challenges and Opportunities for Modulating Tumor Metabolic and Immunological Landscape

Huocheng Yang, Xuemei Yao, Yingqi Liu, Xinkun Shen, Menghuan Li and Zhong Luo

ACS Nano, 2023, 17, 15328
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Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors

Kuojun Zhang, Ke Ye, He Tang, Zhihao Qi, Tianyu Wang, Jie Mao, Xiangyu Zhang and Sheng Jiang

J. Med. Chem., 2023, 66, 4378
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PROTACable Is an Integrative Computational Pipeline of 3-D Modeling and Deep Learning To Automate the De Novo Design of PROTACs

Hazem Mslati, Francesco Gentile, Mohit Pandey, Fuqiang Ban and Artem Cherkasov

J. Chem. Inf. Model., 2024, 64, 3034
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Tuning ubiquitin transfer by RING E3 ubiquitin ligases through the linchpin residue

Mark A Nakasone, Lori Buetow, Mads Gabrielsen, Syed F Ahmed, Karolina A Majorek, Gary J Sibbet, Brian O Smith and Danny T Huang

Life Sci. Alliance, 2025, 8, e202503394
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Targeting ferroptosis: Paving new roads for drug design and discovery

Yilin Gu, Yizhe Li, Jiaxing Wang, Lele Zhang, Jifa Zhang and Yuxi Wang

European Journal of Medicinal Chemistry, 2023, 247, 115015
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Between Theory and Practice: Computational/Experimental Integrated Approaches to Understand the Solubility and Lipophilicity of PROTACs

Andrea Venturi, Stefano Di Bona, Jenny Desantis, Michela Eleuteri, Matteo Bartalucci, Massimo Baroni, Paolo Benedetti, Laura Goracci and Gabriele Cruciani

J. Med. Chem., 2024, 67, 16355
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Aptamer-Hytac Chimeras for Targeted Degradation of SARS-CoV-2 Spike-1

Carme Fàbrega, Núria Gallisà-Suñé, Alice Zuin, Juan Sebastián Ruíz, Bernat Coll-Martínez, Gemma Fabriàs, Ramon Eritja and Bernat Crosas

Cells, 2024, 13, 1767
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ClickRNA-PROTAC for Tumor-Selective Protein Degradation and Targeted Cancer Therapy

Xucong Teng, Xuan Zhao, Yicong Dai, Xiangdong Zhang, Qiushuang Zhang, Yuncong Wu, Difei Hu and Jinghong Li

J. Am. Chem. Soc., 2024, 146, 27382
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Tandem‐Activatable PROTAC Prodrug for Tumor Biomarker‐Driven Near‐Infrared Opto‐Proteolysis

Xiaoyan Lu, Xiaoning Wang, Hanwen Liao, Baitong Sha, Yan Zhang and Jinbo Li

Angewandte Chemie, 2025, 137
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Discovery of ERD-3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity

Zhixiang Chen, Biao Hu, Rohan Kalyan Rej, Dimin Wu, Ranjan Kumar Acharyya, Mingliang Wang, Tianfeng Xu, Jianfeng Lu, Hoda Metwally, Yu Wang, Donna McEachern, Longchuan Bai, Christina L. Gersch, Meilin Wang, Wenjing Zhang, Qiuxia Li, Bo Wen, Duxin Sun, James M. Rae and Shaomeng Wang

J. Med. Chem., 2023, 66, 12559
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P4ward: An Automated Modeling Platform for Protac Ternary Complexes

Paula Jofily and Subha Kalyaanamoorthy

J. Chem. Inf. Model., 2025, 65, 8806
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Novel technologies are turning a dream into reality: conditionally replicating viruses as vaccines

Yan-Dong Tang, Changqing Yu and Xue-Hui Cai

Trends in Microbiology, 2024, 32, 292
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IgE-FcεRI protein–protein interaction as a therapeutic target against allergic asthma: An updated review

Yan-Jun Liu, Hui-Ying Wang, Ran Wang, Jing Yu, Jin-Jin Shi, Ru-Yi Chen, Guan-Jun Yang and Jiong Chen

International Journal of Biological Macromolecules, 2025, 284, 138099
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Unveiling New Triazoloquinoxaline‐Based PROTACs Designed for the Selective Degradation of the ncBAF Chromatin Remodeling Subunit BRD9

Martina Pierri, Guglielmo Bove, Erica Gazzillo, Ester Colarusso, Francesca Scala, Giacomo Pepe, Stefania Terracciano, Maria Giovanna Chini, Nicla Simonelli, Ines Bruno, Angela Nebbioso, Pietro Campiglia, Giuseppe Bifulco, Lucia Altucci, Nunzio Del Gaudio and Gianluigi Lauro

Chemistry A European J, 2025, 31
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Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

Chunrong Yang, Yuchen Yang, Yujie Li, Qiankun Ni and Jinghong Li

J. Am. Chem. Soc., 2023, 145, 385
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Small molecules targeting selected histone methyltransferases (HMTs) for cancer treatment: Current progress and novel strategies

Deping Li, Xiaopeng Peng, Zhihao Hu, Shuqing Li, Jianjun Chen and Wanyi Pan

European Journal of Medicinal Chemistry, 2024, 264, 115982
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Clozapine as an E3 Ligand for PROTAC Technology

Reina Takano, Nobumichi Ohoka, Takashi Kurohara, Noriaki Arakawa, Kenji Ohgane, Takao Inoue, Hidetomo Yokoo and Yosuke Demizu

ACS Med. Chem. Lett., 2025, 16, 258
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New drug discovery and development from natural products: Advances and strategies

Yixin Wang, Fan Wang, Wenxiu Liu, Yifei Geng, Yahong Shi, Yu Tian, Bin Zhang, Yun Luo and Xiaobo Sun

Pharmacology & Therapeutics, 2024, 264, 108752
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SMARCA2 protein: Structure, function and perspectives of drug design

Zhaolin Guo, Peng Wang, Yuxuan Han, Sisi Jiang, Xinyu Yang and Shuang Cao

European Journal of Medicinal Chemistry, 2025, 286, 117319
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Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs

Donglu Zhang, Bin Ma, Peter S. Dragovich, Li Ma, Shu Chen, Eugene C. Chen, Xiaofen Ye, Joyce Liu, Jennifer Pizzano, Elizabeth Bortolon, Emily Chan, Xing Zhang, Yi-Chen Chen, Elizabeth S. Levy, Robert L. Yauch, S. Cyrus Khojasteh and Cornelis E. C. A. Hop

Commun Med, 2024, 4
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Design and Evaluation of PROTACs Targeting Acyl Protein Thioesterase 1

Luís A. R. Carvalho, Bárbara B. Sousa, Daniel Zaidman, Hannah Kiely‐Collins and Gonçalo J. L. Bernardes

ChemBioChem, 2024, 25
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Drugs from drugs: New chemical insights into a mature concept

Eloy Lozano Baró, Federica Catti, Carolina Estarellas, Ouldouz Ghashghaei and Rodolfo Lavilla

Drug Discovery Today, 2024, 29, 104212
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Co-delivery of PROTAC and siRNA via novel liposomes for the treatment of malignant tumors

Wenkai Zhang, Yi Jin, Jiayu Wang, Muge Gu, Yue Wang, Xiangqi Zhang, Yihui Zhang, Wei Yu, Yao Liu, Wei-En Yuan and Jing Su

Journal of Colloid and Interface Science, 2025, 678, 896
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Discovery of a Novel Non-invasive AR PROTAC Degrader for the Topical Treatment of Androgenetic Alopecia

Xinfei Mao, Weitong Hu, Mingfei Wu, Yuyuan Jin, Jingyi Zhao, Yihua Xu, Bizhi Li, Wentao Wang, Yiquan Wu, Jingyu Zhang, Ao Pang, Yuheng Jin, Tianyuan Zhang, Wenhai Huang, Jinxin Che, Jianqing Gao and Xiaowu Dong

J. Med. Chem., 2024, 67, 22218
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How to exploit the recycling system of a cell

Sasha L Evans, Bethany A Haynes, Delia Capatina and Rivka L Isaacson

eLife, 2025, 14
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Designing Bioorthogonal Reactions for Biomedical Applications

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Research, 2023, 6
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The 17th EFMC Short Course on Medicinal Chemistry on Small Molecule Protein Degraders

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ChemMedChem, 2023, 18
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Luciferase- and HaloTag-based reporter assays to measure small-molecule-induced degradation pathway in living cells

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Nat Protoc, 2024, 19, 2317
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Discovery of CW-3308 as a Potent, Selective, and Orally Efficacious PROTAC Degrader of BRD9

Changwei Wang, Mi Wang, Yu Wang, Rohan Kalyan Rej, Angelo Aguilar, Tianfeng Xu, Longchuan Bai, Jelena Tošović, Donna McEachern, Qiuxia Li, Farzad Sarkari, Bo Wen, Duxin Sun and Shaomeng Wang

J. Med. Chem., 2024, 67, 14125
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Chemical dissection of selective myeloid leukemia-1 inhibitors: How they were found and evolved

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European Journal of Medicinal Chemistry, 2025, 283, 117168
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Physicochemical Property Determinants of Oral Absorption for PROTAC Protein Degraders

Keith R. Hornberger and Erika M. V. Araujo

J. Med. Chem., 2023, 66, 8281
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A Covalent Self-Reporting Peptide Degrader Enables Real-Time Monitoring of Targeted Protein Degradation In Vivo

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J. Am. Chem. Soc., 2025, 147, 27862
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A Validated Liquid Chromatography–Tandem Mass Spectrometry Assay for the Determination of NX‐5948 in Beagle Dog Plasma: Application to a Pharmacokinetic Study

Fang Wang, Wenfei Sun, Zheheng Ma and Furui Chu

Biomedical Chromatography, 2025, 39
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Precise Conformational Control Yielding Highly Potent and Exceptionally Selective BRD4 Degraders with Strong Antitumor Activity

Jiantao Hu, Biao Hu, Fuming Xu, Mi Wang, Chong Qin, Donna McEachern, Jeanne Stuckey and Shaomeng Wang

J. Med. Chem., 2023, 66, 8222
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Recent Advances in Nanomedicine: Cutting-Edge Research on Nano-PROTAC Delivery Systems for Cancer Therapy

Xiaoqing Wu, Yueli Shu, Yao Zheng, Peichuan Zhang, Hanwen Cong, Yingpei Zou, Hao Cai and Zhengyu Zha

Pharmaceutics, 2025, 17, 1037
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Auto-RapTAC: A Versatile and Sustainable Platform for the Automated Rapid Synthesis and Evaluation of PROTAC

Jiexuan Chen, Mingfei Wu, Jun Mo, Ju Hong, Wei Wang, Yuheng Jin, Xinfei Mao, Xueyan Liao, Kailin Li, Xiaoli Yu, Sikang Chen, Shenxin Zeng, Wenhai Huang, Hongxia Xu, Jian Wu, Ji Cao, Yubo Zhou, Meidan Ying, Chengliang Zhu, Qiaojun He, Bo Zhang, Nengming Lin, Xiaowu Dong and Jinxin Che

J. Med. Chem., 2025, 68, 8010
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Nano Proteolysis Targeting Chimeras (PROTACs) with Anti‐Hook Effect for Tumor Therapy

Ni‐Yuan Zhang, Da‐Yong Hou, Xing‐Jie Hu, Jian‐Xiao Liang, Man‐Di Wang, Zhang‐Zhi Song, Li Yi, Zhi‐Jia Wang, Hong‐Wei An, Wanhai Xu and Hao Wang

Angewandte Chemie, 2023, 135
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Progress of proteolysis-targeting chimeras (PROTACs) delivery system in tumor treatment

Lianlian Fan, Weifang Tong, Anhui Wei and Xupeng Mu

International Journal of Biological Macromolecules, 2024, 275, 133680
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In Vitro ADME Profiling of PROTACs: Successes, Challenges, and Lessons Learned from Analysis of Clinical PROTACs from a Diverse Physicochemical Space

Abhishek Srivastava, Andy Pike, Magda Swedrowska, Samuel Nash and Ken Grime

J. Med. Chem., 2025, 68, 9584
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Monoselective Histone Deacetylase 6 PROTAC Degrader Shows In Vivo Tractability

Harsimran K. Garcha, Olasunkanmi O. Olaoye, Abootaleb Sedighi, Daniel Pölöske, Pearla Hariri, Wenlong Yu, Diaaeldin I. Abdallah, Richard Moriggl, Elvin D. de Araujo and Patrick T. Gunning

J. Med. Chem., 2025, 68, 6165
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Designing the Proteome with Chemical Tools: Degrons and Beyond

Laurence J. Seabrook, Catherine R. Livelo and Lauren V. Albrecht

ChemBioChem, 2025, 26
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Structure, functions, and recent advances in the development of SIRT2 inhibitors

Junxin Xue, Xuben Hou and Hao Fang

Pharmaceutical Science Advances, 2023, 1, 100010
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Tandem‐Activatable PROTAC Prodrug for Tumor Biomarker‐Driven Near‐Infrared Opto‐Proteolysis

Xiaoyan Lu, Xiaoning Wang, Hanwen Liao, Baitong Sha, Yan Zhang and Jinbo Li

Angew Chem Int Ed, 2025, 64
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Development of Nitroso-Based Probes for Labeling and Regulation of RAS Proteins in Cancer Cells via Sequential Ene-Ligation and Oxime Condensation

Yuanyuan Li, Hongling Zhou, Huili Liu, Youfang Gan, Yaying Zheng, Jia Sheng and Rui Wang

J. Org. Chem., 2023, 88, 1762
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Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs

Christian Steinebach, Aleša Bricelj, Arunima Murgai, Izidor Sosič, Luca Bischof, Yuen Lam Dora Ng, Christopher Heim, Samuel Maiwald, Matic Proj, Rabea Voget, Felix Feller, Janez Košmrlj, Valeriia Sapozhnikova, Annika Schmidt, Maximilian Rudolf Zuleeg, Patricia Lemnitzer, Philipp Mertins, Finn K. Hansen, Michael Gütschow, Jan Krönke and Marcus D. Hartmann

J. Med. Chem., 2023, 66, 14513
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Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer

Xufen Yu, Dongxu Li, Jithesh Kottur, Huen Suk Kim, Laura E. Herring, Yao Yu, Ling Xie, Xiaoping Hu, Xian Chen, Ling Cai, Jing Liu, Aneel K. Aggarwal, Gang Greg Wang and Jian Jin

J. Med. Chem., 2023, 66, 16168
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A Multi-Split-and-Mix Platform for a Variety of Targeted Protein Degradation

Yuechen Wang, Qinhong Luo, Yun Xing, Rui Wang, Fenfang Yang, Weifan Cao, Zigang Li and Feng Yin

ACS Chem. Biol., 2025
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Targeting the STAT3 pathway with STAT3 degraders

Zhijie Wang, Xiaotong Liao, Haiqi He, Xia Guo and Jianjun Chen

Trends in Pharmacological Sciences, 2024, 45, 811
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Supramolecular artificial Nano-AUTACs enable tumor-specific metabolism protein degradation for synergistic immunotherapy

Yazhen Wang, Lianyi Yang, Chenxing Yan, Yufan Du, Tinghua Li, Wenqing Yang, Lei Lei, Bin He, Huile Gao, Nicholas A. Peppas and Jun Cao

Sci. Adv., 2024, 10
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Exosome-mediated intercellular communication and PROTACs delivery: A dual approach for precision therapy in colon cancer

Popat Mohite, Abhijeet Puri, Shubham Munde, Vaishnavi Yadav, Nobendu Mukerjee, Riteshkumar Patil, Nihar Mahindrakar, G.V. Siva Prasad, Rajni Verma and Aashna Sinha

Journal of Drug Delivery Science and Technology, 2025, 105, 106596
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Ultrasound-Activated PROTAC Prodrugs Overcome Immunosuppression to Actuate Efficient Deep-Tissue Sono-Immunotherapy in Orthotopic Pancreatic Tumor Mouse Models

Ye Liu, Haiyang Wang, Mengchao Ding, Wang Yao, Kewei Wang, Ihsan Ullah, Emil Bulatov and Youyong Yuan

Nano Lett., 2024, 24, 8741
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Understanding the role of BRD8 in human carcinogenesis

Kiyoshi Yamaguchi, Saya Nakagawa and Yoichi Furukawa

Cancer Science, 2024, 115, 2862
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Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design

Dazhao Mi, Yuzhan Li, Haijun Gu, Yan Li and Yihua Chen

European Journal of Medicinal Chemistry, 2023, 256, 115444
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Precision-engineered PROTACs minimize off-tissue effects in cancer therapy

Jianghua Shi, Luo Wang, Xuanwei Zeng, Chengzhi Xie, Zhaowei Meng, Anahit Campbell, Lulu Wang, Heli Fan and Huabing Sun

Front. Mol. Biosci., 2024, 11
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Near-Infrared-Activatable PROTAC Nanocages for Controllable Target Protein Degradation and On-Demand Antitumor Therapy

Qi He, Liming Zhou, Daxin Yu, Ren Zhu, Yue Chen, Mingbo Song, Xintong Liu, Yixian Liao, Tong Ding, Wenpei Fan and Wenying Yu

J. Med. Chem., 2023, 66, 10458
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Targeted protein degradation as an antiviral approach

Antara Chakravarty and Priscilla L. Yang

Antiviral Research, 2023, 210, 105480
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Targeting oncogenic transcriptional factor c-myc by oligonucleotide PROTAC for the treatment of hepatocellular carcinoma

Min Ai, Hulin Ma, Jianhua He, Fuyan Xu, Yue Ming, Zixia Ye, Qingquan Zheng, Dongdong Luo, Kaichuan Yang, Jiao Li, Chunlai Nie, Wenchen Pu and Yong Peng

European Journal of Medicinal Chemistry, 2024, 280, 116978
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Glycoconjugates: Synthesis, Functional Studies, and Therapeutic Developments

Sachin S. Shivatare, Vidya S. Shivatare and Chi-Huey Wong

Chem. Rev., 2022, 122, 15603
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Research Advances in Chaperone-Mediated Autophagy (CMA) and CMA-Based Protein Degraders

Zhaoping Pan, Xiaowei Huang, Mingxia Liu, Xian Jiang and Gu He

J. Med. Chem., 2025, 68, 2314
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Discovery of Effective Dual PROTAC Degraders for Neurodegenerative Disease-Associated Aggregates

Wentao Zhu, Wenqian Zhang, Jian Chen, Yichen Tong, Fang Xu and Jiyan Pang

J. Med. Chem., 2024, 67, 3448
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Site-resolved assessment of targeted protein degradation

Ricardo Moreno-Ballesteros, Thomas Pembridge, Gaurav Beniwal and Satpal Virdee

Cell Chemical Biology, 2025, 32, 969
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Structure-Guided Design of ISOX-DUAL-Based Degraders Targeting BRD4 and CBP/EP300: A Case of Degrader Collapse

Anthony K. Edmonds, Dimitrios-Ilias Balourdas, Graham P. Marsh, Robert Felix, Bradley Brasher, Jeff Cooper, Cari Graber-Feesl, Madhu Kollareddy, Karim Malik, Helen Stewart, Timothy J. T. Chevassut, Ella Lineham, Simon Morley, Oleg Fedorov, James Bennett, Mohan B. Rajasekaran, Samuel Ojeda, Drew A. Harrison, Christopher J. Ott, Andreas C. Joerger, Hannah J. Maple and John Spencer

J. Med. Chem., 2025, 68, 9638
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Albumin-encapsulated HSP90-PROTAC BP3 nanoparticles not only retain protein degradation ability but also enhance the antitumour activity of BP3 in vivo

Qingna Jiang, Yan Hu, Quanyu Liu, Yuanling Tang, Xinhua Wu, Jingwen Liu, Guihui Tu, Ge Li, Xiaoqing Lin, Minghui Qu, Yajuan Cai, Xiuwang Huang, Jianhua Xu, Yanping Deng, Zhuo Chen and Lixian Wu

Journal of Drug Targeting, 2023, 31, 411
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Targeting Moonlighting Enzymes in Cancer

Chunxu Lin, Mingyang Yu, Ximei Wu, Hui Wang, Min Wei and Luyong Zhang

Molecules, 2024, 29, 1573
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Design, Synthesis, and Activity Evaluation of BRD4 PROTAC Based on Alkenyl Oxindole-DCAF11 Pair

Man Zhao, Wenjing Ma, Jinyi Liang, Yubao Xie, Tianzi Wei, Ming Zhang, Jiajie Qin, Lingyin Lao, Ruilin Tian, Haiqiang Wu, Jin Cheng, Min Li, Yuyang Liu, Liang Hong and Guofeng Li

J. Med. Chem., 2024, 67, 19428
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Cell-Specific Degradation of Histone Deacetylase Using Warhead-Caged Proteolysis Targeting Chimeras

Qi Jia, Yue Zhang, Feng Liu, Wanrong Dong, Lei Zhu, Fenglin Wang and Jian-Hui Jiang

Anal. Chem., 2023, 95, 16474
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A compact, versatile drug-induced splicing switch system with minimal background expression

Yue Chi, Xuan Lu, Shuangpeng Li, Jinling Wang, Jiahui Xi, Xiaoqing Zhou, Chengcheng Tang, Min Chen, Hui Yuan, Shuo Lin, Yingying Xiao, Liangxue Lai and Qingjian Zou

Cell Reports Methods, 2024, 4, 100842
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Intercepting the Downstream of the Estrogen Receptor Signaling Pathway: Discovery of a Potent and Efficient SRC-3 PROTAC Degrader for Overcoming Endocrine Resistance Breast Cancer

Jinsen Liang, Dandan Wang, Yihe Wu, Jiahao Shi, Baohua Xie, Ruijing Xiao, Jian Ni, Chao Wang, Chune Dong, Hong-Bing Shu, Shu Li and Hai-Bing Zhou

J. Med. Chem., 2025, 68, 11516
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Exploiting Cancer Vulnerabilities by Blocking of the DHODH and GPX4 Pathways: A Multifunctional Bodipy/PROTAC Nanoplatform for the Efficient Synergistic Ferroptosis Therapy

Lang Yao, Na Yang, Wei Zhou, Mahmood Hassan Akhtar, Weiping Zhou, Chang Liu, Shuang Song, Ying Li, Wenzhao Han and Cong Yu

Adv Healthcare Materials, 2023, 12
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First ATG101-recruiting small molecule degrader for selective CDK9 degradation via autophagy–lysosome pathway

Ye Zhong, Jing Xu, Huiying Cao, Jie Gao, Shaoyue Ding, Zhaohui Ren, Huali Yang, Yili Sun, Maosheng Cheng, Jia Li and Yang Liu

Acta Pharmaceutica Sinica B, 2025, 15, 2612
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Generation of tau dephosphorylation-targeting chimeras for the treatment of Alzheimer’s disease and related tauopathies

Jingfen Su, Yue Xiao, Linyu Wei, Huiyang Lei, Fei Sun, Weixia Wang, Jun Yin, Rui Xiong, Shihong Li, Pei Zhang, Ying Zhou, Xiaochuan Wang, Jie Zheng and Jian-Zhi Wang

Science Bulletin, 2024, 69, 1137
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Identification of Potential DCAF1 Inhibitors Through Virtual Screening Based on Molecular Docking and Molecular Dynamics Simulations

Bing Liao, Jing Chen, Qing Ye, Gang Cheng and Lu‐Ping Qin

ChemistrySelect, 2025, 10
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Revealing the multiple faces of LRG1: gene expression, structure, function, and therapeutic potential

Ding Wang, Di Di, Bo Jiang, Yunlong Wang, Zhenqi Jiang, Yuchen Jing, Huizhe Wu and Shijie Xin

Journal of Advanced Research, 2025
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Molecular Design of Novel Protein-Degrading Therapeutics Agents Currently in Clinical Trial

Ela Kacin and Raj Nayan Sewduth

Pharmaceutics, 2025, 17, 744
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Degradation of extracellular and membrane proteins in targeted therapy: Status quo and quo vadis

Zhenzhen Li, Siyue Ma, Shuxin Zhang, Zhao Ma, Lupei Du and Minyong Li

Drug Discovery Today, 2023, 28, 103716
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Unconventional PROTACs for Targeted Protein Degradation in Cancer Therapy

Xu Zhang, Zhangzhi Song, Xinyu Zhang, Jianhua Zou, Guocan Yu, Xiaoyuan Chen and Sheng Wang

Angewandte Chemie, 2025, 137
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Ultrasound Controllable Release of Proteolysis Targeting Chimeras for Triple-Negative Breast Cancer Treatment

Hongye He, Feng Li, Rui Tang, Nianhong Wu, Ying Zhou, Yuting Cao, Can Wang, Li Wan, Yang Zhou, Hua Zhuang and Pan Li

Biomater Res, 2024, 2024
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Discovery of the First Potent, Selective, and In Vivo Efficacious Polo-like Kinase 4 Proteolysis Targeting Chimera Degrader for the Treatment of TRIM37-Amplified Breast Cancer

Yin Sun, Yanli Xue, Pengkun Sun, Shuyi Mu, Hongbing Liu, Yu Sun, Lin Wang, Jingkai Wang, Tianxiao Wu, Wenbo Yin, Qiaohua Qin, Yixiang Sun, Nian Liu, Hanxun Wang, Huali Yang, Dongmei Zhao and Maosheng Cheng

J. Med. Chem., 2023, 66, 8200
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DiPTAC: A degradation platform via directly targeting proteasome

Yutong Tu, Qian Yu, Mengna Li, Lixin Gao, Jialuo Mao, Jingkun Ma, Xiaowu Dong, Jinxin Che, Chong Zhang, Linghui Zeng, Huajian Zhu, Jiaan Shao, Jingli Hou, Liming Hu, Bingbing Wan, Jia Li, Yubo Zhou and Jiankang Zhang

Acta Pharmaceutica Sinica B, 2025, 15, 661
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Role of exchange proteins directly activated by cAMP signaling in vascular remodeling

Xiaodong Cheng, Hua Liu, Wenbo Zhang, Wenli Yang and Fang Mei

Pharmacological Reviews, 2025, 77, 100078
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Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2

Deborah Grifagni, Elena Lenci, Alessia De Santis, Andrea Orsetti, Carlo Giorgio Barracchia, Filomena Tedesco, Raffaele Bellini Puglielli, Francesca Lucarelli, Angela Lauriola, Michael Assfalg, Francesca Cantini, Vito Calderone, Daniele Guardavaccaro, Andrea Trabocchi, Mariapina D’Onofrio and Simone Ciofi-Baffoni

ACS Med. Chem. Lett., 2024, 15, 250
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An updated patent review of BRD4 degraders

Zonghui Ma, Cun Zhang, Andrew A. Bolinger and Jia Zhou

Expert Opinion on Therapeutic Patents, 2024, 34, 929
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Advancing Cancer Immunotherapy through Engineering New PD-L1 Degraders: A Comprehensive Study from Small Molecules to PD-L1-Specific Peptide–Drug Conjugates

Zekun Zeng, Zhiwei Yang, Chenghao Li, Shujing Liu, Wei Wei, Ye Zhou, Simeng Wang, Mengjun Sui, Mengdan Li, Shumei Lin, Yangyang Cheng and Peng Hou

J. Med. Chem., 2024, 67, 19216
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Development and crystal structures of a potent second-generation dual degrader of BCL-2 and BCL-xL

Digant Nayak, Dongwen Lv, Yaxia Yuan, Peiyi Zhang, Wanyi Hu, Anindita Nayak, Eliza A. Ruben, Zongyang Lv, Patrick Sung, Robert Hromas, Guangrong Zheng, Daohong Zhou and Shaun K. Olsen

Nat Commun, 2024, 15
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Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma

Qi Chang, Jiayi Li, Yue Deng, Ruilin Zhou, Bingwei Wang, Yujie Wang, Mingming Zhang, Xun Huang and Yingxia Li

J. Med. Chem., 2024, 67, 2466
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Two-Photon Photodegradation of E3 Ubiquitin Ligase Cereblon by a Ru(II) Complex: Inducing Ferroptosis in Cisplatin-Resistant Tumor Cells

Xinlin Lin, Mengsi Zheng, Kai Xiong, Fa Wang, Yu Chen, Liangnian Ji and Hui Chao

J. Med. Chem., 2024, 67, 8372
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Targeted Degradation of the Estrogen Receptor α through Unconventional Coactivator Binding Site (CBS)

Yubo Wang, Baohua Xie, Xiaofei Deng, Chune Dong and Hai-Bing Zhou

J. Med. Chem., 2025, 68, 13640
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Programmable Circular Multivalent Nanobody‐Targeting Chimeras (mNbTACs) for Multireceptor‐Mediated Protein Degradation and Targeted Drug Delivery

Shiqi Jiang, Xinru Lv, Zhenlin Ouyang, Hongli Chi, Yuchen Zeng, Yani Wang, Jiaxuan He, Jinling Chen, Jingyi Chen, Keli An, Ming Cheng, Yurong Wen, Juan Li and Penghui Zhang

Angew Chem Int Ed, 2024, 63
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Enzyme‐Activated Orthogonal Proteolysis Chimeras for Tumor Microenvironment‐Responsive Immunomodulation

Caixia Sun, Songhan Liu, Jun Wei Lau, Hanyu Yang, Yun Chen and Bengang Xing

Angew Chem Int Ed, 2025, 64
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PROTAC-DB 3.0: an updated database of PROTACs with extended pharmacokinetic parameters

Jingxuan Ge, Shimeng Li, Gaoqi Weng, Huating Wang, Meijing Fang, Huiyong Sun, Yafeng Deng, Chang- Yu Hsieh, Dan Li and Tingjun Hou

Nucleic Acids Research, 2025, 53, D1510
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PROTAC-loaded nanocapsules degrading BRD4 for radio-chemotherapy sensitization in glioblastoma

Yun Guo, Mingzhu Fang, Shilin Zhang, Zheng Zhou, Zonghua Tian, Haoyu You, Yun Chen, Jingyi Zhou, Xiaobao Yang, Yunke Bi, Chen Jiang and Tao Sun

Acta Pharmaceutica Sinica B, 2025
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A prospective therapeutic strategy: GPX4-targeted ferroptosis mediators

Jia-Yu Qian, Chao-Yuan Lou, Yi-Li Chen, Lie-Feng Ma, Wei Hou and Zha-Jun Zhan

European Journal of Medicinal Chemistry, 2025, 281, 117015
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Targeting kelch-like (KLHL) proteins: achievements, challenges and perspectives

Yangguo Zhou, Qiong Zhang, Ziquan Zhao, Xiuqi Hu, Qidong You and Zhengyu Jiang

European Journal of Medicinal Chemistry, 2024, 269, 116270
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Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7)

Wenzhi Ji, Guangyan Du, Jie Jiang, Wenchao Lu, Caitlin E. Mills, Linjie Yuan, Fen Jiang, Zhixiang He, Gary A. Bradshaw, Mirra Chung, Zixuan Jiang, Woong Sub Byun, Stephen M. Hinshaw, Tinghu Zhang and Nathanael S. Gray

European Journal of Medicinal Chemistry, 2024, 276, 116613
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BRD4 PROTAC degrader MZ1 exhibits anti-B-cell acute lymphoblastic leukemia effects via targeting CCND3

Li Ma, Jianwei Wang, Yang Yang, Jun Lu, Jing Ling, Xinran Chu, Zimu Zhang, Yanfang Tao, Xiaolu Li, Yuanyuan Tian, Zhiheng Li, Yongping Zhang, Xu Sang, Lihui Lu, Xiaomei Wan, Kunlong Zhang, Yanling Chen, Juanjuan Yu, Ran Zhuo, Shuiyan Wu, Jian Pan, Xiuxia Zhou, Yixin Hu and Shaoyan Hu

Hematology, 2023, 28
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In Vivo Self‐Assembly of PROTACs by Bioorthogonal Chemistry for Precision Cancer Therapy

Shaowen Xie, Jingjie Zhu, Yihan Peng, Fangyi Zhan, Feiyan Zhan, Chen He, Dazhi Feng, Jia Xie, Jingyu Liu, Huajian Zhu, Hong Yao, Jinyi Xu, Zhigui Su and Shengtao Xu

Angew Chem Int Ed, 2025, 64
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A Mechanistic Pharmacodynamic Modeling Framework for the Assessment and Optimization of Proteolysis Targeting Chimeras (PROTACs)

Robin Haid and Andreas Reichel

Pharmaceutics, 2023, 15, 195
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Metal Modulation: An Effortless Tactic for Refining Photoredox Catalysis in Living Cells

Le Yu, Kyung-Woo Lee, Yu-Qiang Zhao, Yunjie Xu, Ying Zhou, Mingle Li and Jong Seung Kim

Inorg. Chem., 2023, 62, 18767
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Degradation of Rat Sarcoma Proteins Targeting the Post-Translational Prenyl Modifications via Cascade Azidation/Fluorination and Click Reaction

Hongling Zhou, Youfang Gan, Yuanyuan Li, Xiaoqian Chen, Yuyang Guo and Rui Wang

J. Med. Chem., 2023, 66, 7243
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Dual SLIPT–A Lipid Mimic to Enable Spatiotemporally Defined, Sequential Protein Dimerization

Kristina V. Bayer, Maedeh Taeb, Birgit Koch, Shige H. Yoshimura and Richard Wombacher

ACS Chem. Biol., 2025, 20, 1038
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M1/M2 macrophage-targeted nanotechnology and PROTAC for the treatment of atherosclerosis

Yupeng Ma, Xiaofan Yang, Ke Ning and Haidong Guo

Life Sciences, 2024, 352, 122811
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Unconventional PROTACs for Targeted Protein Degradation in Cancer Therapy

Xu Zhang, Zhangzhi Song, Xinyu Zhang, Jianhua Zou, Guocan Yu, Xiaoyuan Chen and Sheng Wang

Angew Chem Int Ed, 2025, 64
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Light‐Triggered PROTAC Nanoassemblies for Photodynamic IDO Proteolysis in Cancer Immunotherapy

Jiwoong Choi, Byeongmin Park, Jung Yeon Park, Dongwon Shin, Sangmin Lee, Hong Yeol Yoon, Kwangmeyung Kim, Sun Hwa Kim, Yongju Kim, Yoosoo Yang and Man Kyu Shim

Advanced Materials, 2024, 36
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New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives

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Acta Materia Medica, 2024, 3
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Design, synthesis, and biological evaluation of novel BTK-targeting proteolysis targeting chimeras (PROTACs) with enhanced pharmacokinetic properties

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European Journal of Medicinal Chemistry, 2025, 289, 117420
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Molecular engineering tools for the development of vaccines against infectious diseases: current status and future directions

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Heterobifunctional Ligase Recruiters Enable pan-Degradation of Inhibitor of Apoptosis Proteins

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Cyclic nucleotide phosphodiesterases as drug targets

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Semiconducting Polymers for Cancer Immunotherapy

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Design of FK866-Based Degraders for Blocking the Nonenzymatic Functions of Nicotinamide Phosphoribosyltransferase

Tiangong Lu, Fangfang Chen, Jian Yao, Zixuan Bu, Armita Kyani, Benji Liang, Shaoting Chen, Yuxiang Zheng, Hong Liang, Nouri Neamati and Yanghan Liu

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Discovery of DHODH PROTAC degraders with anti-SARS-CoV-2 and influenza virus activity

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Chinese Chemical Letters, 2025, 111751
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Development of a versatile system for evaluating the target protein degradation activity of novel ubiquitin ligases utilizing existing PROTACs

Shinya Sato, Mei Matsukawa, Masaaki Takemoto, Takumi Okamoto, Atsushi Saito, Issei Omura, Koji Matsuhisa, Hiroaki Ikeda, Kazunori Imaizumi and Masayuki Kaneko

Biochemical and Biophysical Research Communications, 2025, 749, 151370
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Chemical Proteomics Identifies RBBP7 as a New E3 Ligase Supporting Targeted Protein Degradation

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Angew Chem Int Ed, 2025
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Discovery of an activatable near-infrared fluorescent and theranostic PROTAC for tumor-targeted detecting and degrading of BRD4

Keliang Li, Guoqiang Dong, Shanchao Wu and Chunquan Sheng

Chinese Chemical Letters, 2025, 36, 110280
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Aptamers: Promising Reagents in Biomedicine Application

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Advanced Biology, 2024, 8
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RIPTACs for Precision Cancer Therapy: A Novel Modality with the Inspiration of HLD-0915 as the First Candidate in Clinical Trials

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Targeted Protein Degraders- The Druggability Perspective

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Journal of Pharmaceutical Sciences, 2024, 113, 539
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Protein degradation kinetics measured by microinjection and live-cell fluorescence microscopy

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Sci Rep, 2024, 14
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Nanotechnology‐Enabled Targeted Protein Degradation for Cancer Therapeutics

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Degradation of Hexokinase 2 Blocks Glycolysis and Induces GSDME-Dependent Pyroptosis to Amplify Immunogenic Cell Death for Breast Cancer Therapy

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J. Med. Chem., 2023, 66, 8464
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Toward effective Atg8‐based ATTECs: Approaches and perspectives

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Current advances and development strategies of orally bioavailable PROTACs

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European Journal of Medicinal Chemistry, 2023, 261, 115793
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Recent advances in developing targeted protein degraders

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European Journal of Medicinal Chemistry, 2025, 284, 117212
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A one-pot photocatalytic triazole-based linkerology for PROTACs

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Development of versatile solid-phase methods for syntheses of PROTACs with diverse E3 ligands

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Bioorganic & Medicinal Chemistry, 2023, 86, 117293
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Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer

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Antiviral nanomedicine: Advantages, mechanisms and advanced therapies

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Small molecule approaches to targeting RNA

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Nat Rev Chem, 2024, 8, 120
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Epidermal growth factor receptor PROTACs as an effective strategy for cancer therapy: A review

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Annual review of EGFR inhibitors in 2024

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MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment

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IJMS, 2022, 23, 11068
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Paired Electro‐Synthesis of Remote Amino Alcohols with/in H2O

Xinyue Fang, Xinwei Hu, Quan‐Xin Li, Shao‐Fei Ni and Zhixiong Ruan

Angew Chem Int Ed, 2025, 64
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Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization

Martin P. Schwalm, Andreas Krämer, Anja Dölle, Janik Weckesser, Xufen Yu, Jian Jin, Krishna Saxena and Stefan Knapp

Cell Chemical Biology, 2023, 30, 753
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Reversible in-situ assembly of PROTACs using iminoboronate conjugation

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Pt(IV)-PROTAC Complexes with Synergistic Antitumor Activity and Enhanced Membrane Permeability

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J. Med. Chem., 2025, 68, 8208
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Characterizing the Cooperative Effect of PROTAC Systems with End-Point Binding Free Energy Calculation

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Global landscape of PROTAC: Perspectives from patents, drug pipelines, clinical trials, and licensing transactions

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European Journal of Medicinal Chemistry, 2025, 299, 118055
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Emerging drug design strategies in anti-influenza drug discovery

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Acta Pharmaceutica Sinica B, 2023, 13, 4715
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Radioactive ADME Demonstrates ARV-110’s High Druggability Despite Low Oral Bioavailability

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Research Progress of PROTAC-Degraded CDKs in the Treatment of Breast Cancer

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Discovery of Novel PROTAC SIRT6 Degraders with Potent Efficacy against Hepatocellular Carcinoma

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Multi-Faceted Roles of DNAJB Protein in Cancer Metastasis and Clinical Implications

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IJMS, 2022, 23, 14970
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Hydrophobic tag-based protein degradation: Development, opportunity and challenge

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European Journal of Medicinal Chemistry, 2023, 260, 115741
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Targeted Degradation of Androgen Receptor for the Potential Treatment of Prostate Cancer

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ACS Med. Chem. Lett., 2022, 13, 1558
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Fragment-based drug discovery supports drugging ‘undruggable’ protein–protein interactions

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METTL3 protects METTL14 from STUB1‐mediated degradation to maintain m6A homeostasis

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A Mild and Sustainable Procedure for the Functionalization of Morpholin-2-Ones by Oxidative Imidation Reactions

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Catalysts, 2023, 13, 1072
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Rational Proteolysis Targeting Chimera Design Driven by Molecular Modeling and Machine Learning

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Targeted Protein Degradation Systems: Controlling Protein Stability Using E3 Ubiquitin Ligases in Eukaryotic Species

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Cells, 2024, 13, 175
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HerTACs Enable Tumor‐Selective Lysosomal Degradation of Membrane and Extracellular Proteins via HER2 Trafficking

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Targeting PRMT5 through PROTAC for the treatment of triple-negative breast cancer

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Design and optimization strategies of PROTACs and its Application, Comparisons to other targeted protein degradation for multiple oncology therapies

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STING in cancer immunoediting: Modeling tumor-immune dynamics throughout cancer development

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Patenting perspective of modulators of ClpP endopeptidase: 2019-present

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Design, synthesis and evaluation of the first DYRK1A degrader for promoting the proliferation of pancreatic β-cells

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Chinese Chemical Letters, 2024, 35, 109570
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Targeted protein degradation in hematologic malignancies: clinical progression towards novel therapeutics

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A Wireless Operated Flexible Bioelectronic Microneedle Patch for Actively Controlled Transdermal Drug Delivery

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Advanced Materials, 2025, 37
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Sulfatase-Induced In Situ Formulation of Antineoplastic Supra-PROTACs

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Receptor Elimination by E3 Ubiquitin Ligase Recruitment (REULR): A Targeted Protein Degradation Toolbox

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Use of Aldehyde–Alkyne–Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers

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CsMIEL1 effectively inhibits the accumulation of anthocyanins under low temperatures in tea plants (Camellia sinensis)

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Discovery of a Highly Potent, Selective and Efficacious USP7 Degrader for the Treatment of Acute Lymphoblastic Leukemia

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Modular Assembly of Heterotrifunctional Molecules Enabled by Iodosulfonylation of Allenes and Subsequent Amination

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Discovery of novel 20S proteasome subunit β5 PROTAC degraders as potential therapeutics for pharyngeal carcinoma and Bortezomib-resistant multiple myeloma

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Bioorganic Chemistry, 2024, 153, 107801
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Nanomaterials exert biological effects by influencing the ubiquitin-proteasome system

Zhen Ai, Dan Li, Shuquan Lan and Chao Zhang

European Journal of Medicinal Chemistry, 2025, 282, 116974
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Regulation of programmed cell death by Brd4

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Utilizing aptamers in targeted protein degradation strategies for disease therapy

Lin Li, Songbo Xie, Jun Zhou and Jie Ran

The Journal of Pathology, 2025, 266, 134
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Drug discovery inspired by bioactive small molecules from nature

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Animal Cells and Systems, 2022, 26, 254
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An Oral PROTAC Targeting HPK1 Degradation Potentiates Anti‐Solid Tumor Immunity

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Advancing cancer immunotherapy: Small-Molecule, biomacromolecular, and nanoscale PROTACs targeting PD-L1 for degradation

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Rational Design of Bioorthogonally Activatable PROTAC for Tumor-Targeted Protein Degradation

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Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)

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Clinical Research Progress of BTK Inhibitors in the Treatment of Autoimmune Diseases

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Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders

Nisha Setia, Haider Thaer Abdulhameed Almuqdadi and Mohammad Abid

European Journal of Medicinal Chemistry, 2024, 265, 116041
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Cell Membrane as A Promising Therapeutic Target: From Materials Design to Biomedical Applications

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A highly selective and orally bioavailable casein kinase 1 alpha degrader through p53 signaling pathway targets B-cell lymphoma cells

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YY1 enhances HIF-1α stability in tumor-associated macrophages to suppress anti-tumor immunity of prostate cancer in mice

Wenchao Li, SaiSai Chen, Jian Lu, Weipu Mao, Shiya Zheng, Minhao Zhang, Tiange Wu, Yurui Chen, Kai Lu, Chunyan Chu, Chuanjun Shu, Yue Hou, Xue Yang, Naipeng Shi, Zhijun Chen, Lihua Zhang, Lei Zhang, Rong Na, Ming Chen, Shenghong Ju, Dingxiao Zhang, Yi Ma and Bin Xu

Nat Commun, 2025, 16
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Disrupting the MC1R/α‐MSH‐pCREB‐MITF Axis: Rhein‐based PROTAC D16 as a Potent Melanogenesis Inhibitor

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Targeting bacterial degradation machinery as an antibacterial strategy

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Biochemical Journal, 2023, 480, 1719
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Current strategies for targeting HPK1 in cancer and the barriers to preclinical progress

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Development and Discovery of a Selective Degrader of Casein Kinases 1 δ/ε

Adrian Haag, Václav Němec, Pavlína Janovská, Jana Bartošíková, Bikash Adhikari, Juliane Müller, Martin P. Schwalm, Štěpán Čada, Uli Ohmayer, Henrik Daub, Yeojin Kim, Florian Born, Elmar Wolf, Vítězslav Bryja and Stefan Knapp

J. Med. Chem., 2025, 68, 506
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Enhanced Tumor Targeting and Penetration of Proteolysis-Targeting Chimeras through iRGD Peptide Conjugation: A Strategy for Precise Protein Degradation in Breast Cancer

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Deubiquitinase-Targeting Chimeras (DUBTACs) as a Potential Paradigm-Shifting Drug Discovery Approach

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The Potential of PARP Inhibitors as Antitumor Drugs and the Perspective of Molecular Design

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Development of a nano-targeting chimera for the degradation of membrane and cytoplasmic proteins

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Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research

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J. Med. Chem., 2023, 66, 1700
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Uncovering the Kinetic Characteristics and Degradation Preference of PROTAC Systems with Advanced Theoretical Analyses

Rongfan Tang, Zhe Wang, Sutong Xiang, Lingling Wang, Yang Yu, Qinghua Wang, Qirui Deng, Tingjun Hou and Huiyong Sun

JACS Au, 2023, 3, 1775
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Discovery of LL-K8-22: A Selective, Durable, and Small-Molecule Degrader of the CDK8-Cyclin C Complex

Mingyu Wang, Rongkun Lin, Jiacheng Li, Yuying Suo, Jing Gao, Liping Liu, Liyuan Zhou, Yicheng Ni, Ziqun Yang, Jie Zheng, Jin Lin, Hu Zhou, Cheng Luo and Hua Lin

J. Med. Chem., 2023, 66, 4932
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Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera

Yuan Yan Sin, Aoife Giblin, Aleksandra Judina, Punchita Rujirachaivej, Laura G. Corral, Eliza Glennon, Zhi Xian Tai, Tian Feng, Eduardo Torres, Alina Zorn, Julia Gorelik, Elka Kyurkchieva, Pa Thai Yenchitsomanus, Cathy Swindlehurst, Kyle Chan, David Stirling and George S. Baillie

The FEBS Journal, 2025, 292, 3360
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Structure-based drug design with geometric deep learning

Clemens Isert, Kenneth Atz and Gisbert Schneider

Current Opinion in Structural Biology, 2023, 79, 102548
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From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors

Mladen Koravovic, Anand Mayasundari, Gordana Tasic, Fatemeh Keramatnia, Timothy R. Stachowski, Huarui Cui, Sergio C. Chai, Barbara Jonchere, Lei Yang, Yong Li, Xiang Fu, Ryan Hiltenbrand, Leena Paul, Vibhor Mishra, Jeffery M. Klco, Martine F. Roussel, William CK. Pomerantz, Marcus Fischer, Zoran Rankovic and Vladimir Savic

European Journal of Medicinal Chemistry, 2023, 251, 115246
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Modular Development of Enzyme-Activatable Proteolysis Targeting Chimeras for Selective Protein Degradation and Cancer Targeting

Yanchi Chen, Lina Zhang, Lincheng Fang, Chengjie Chen, Dong Zhang and Tao Peng

JACS Au, 2024, 4, 2564
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Chimeric Small Molecules for Detouring Drugs into Mitochondria to Engender Apoptosis in Cancer Cells

Tripti Mishra, Abhinav Gautam, Jaypalsing Ingle and Sudipta Basu

ChemBioChem, 2024, 25
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Recent advances of targeting nicotinamide phosphoribosyltransferase (NAMPT) for cancer drug discovery

He Tang, Lin Wang, Tianyu Wang, Jiamei Yang, Shuai Zheng, Jun Tong, Sheng Jiang, Xiangyu Zhang and Kuojun Zhang

European Journal of Medicinal Chemistry, 2023, 258, 115607
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Design, synthesis and biological evaluation of the tumor hypoxia-activated PROTACs bearing caged CRBN E3 ligase ligands

Weiyan Cheng, Shasha Li, Siyuan Han, Ruoyang Miao, Suhua Wang, Chunxia Liu, Han Wei, Xin Tian and Xiaojian Zhang

Bioorganic & Medicinal Chemistry, 2023, 82, 117237
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How many kinases are druggable? A review of our current understanding

Brian Anderson, Peter Rosston, Han Wee Ong, Mohammad Anwar Hossain, Zachary W. Davis-Gilbert and David H. Drewry

Biochemical Journal, 2023, 480, 1331
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Novel Amphiphilic PROTAC with Enhanced Pharmacokinetic Properties for ALK Protein Degradation

Shirui Wang, Zhanzhan Feng, Can Qu, Su Yu, Hongjia Zhang, Rui Deng, Dan Luo, Chunlan Pu, Yan Zhang and Rui Li

J. Med. Chem., 2024, 67, 9842
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Protein degraders - from thalidomide to new PROTACs

Takumi Ito

The Journal of Biochemistry, 2024, 175, 507
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Heparin-Binding Protein Promotes Acute Lung Injury in Sepsis Mice by Blocking the Aryl Hydrocarbon Receptor Signaling Pathway

Kun Ye, Xiang Lin, Tai-Zhi Chen, Long-Hui Wang and Sheng-Xing Liu

JIR, 2024, Volume 17, 2927
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Biospecific Chemistry for Covalent Linking of Biomacromolecules

Li Cao and Lei Wang

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Proteomics‐Based Discovery of First‐in‐Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2)

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Angewandte Chemie, 2023, 135
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TACkling Cancer by Targeting Selective Protein Degradation

María del Mar Noblejas-López, David Tébar-García, Raquel López-Rosa, Ana Alcaraz-Sanabria, Pablo Cristóbal-Cueto, Alejandro Pinedo-Serrano, Lorenzo Rivas-García and Eva M. Galán-Moya

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Overcoming E3 Ligase-Mediated Resistance: Development of Novel Hydrophobic Tagging-Based Degraders Targeting ALK Protein

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New-generation advanced PROTACs as potential therapeutic agents in cancer therapy

Chao Wang, Yujing Zhang, Wujun Chen, Yudong Wu and Dongming Xing

Mol Cancer, 2024, 23
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Can PROTACs cure Leukemia?

Kathleen M. Sakamoto

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HerTACs Enable Tumor‐Selective Lysosomal Degradation of Membrane and Extracellular Proteins via HER2 Trafficking

Shipeng He, Wenjing Huang, Yaojin Zhu, Fei Gao, Yuxin Fang, Jiayi Zhu, Yuhan Bao, Guoqiang Dong and Chunquan Sheng

Angew Chem Int Ed, 2025
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Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression

Zhixiang Chen, Mi Wang, Dimin Wu, Longchuan Bai, Tianfeng Xu, Hoda Metwally, Yu Wang, Donna McEachern, Lijie Zhao, Ruiting Li, John Takyi-Williams, Meilin Wang, Lu Wang, Qiuxia Li, Bo Wen, Duxin Sun and Shaomeng Wang

J. Med. Chem., 2024, 67, 5275
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Targeting focal adhesion kinase (FAK) in cancer therapy: A recent update on inhibitors and PROTAC degraders

Xiao Wang, Na Li, Yun-He Liu, Ji Wu, Qiu-Ge Liu, Jin-Bo Niu, Yan Xu, Chen-Zheng Huang, Sai-Yang Zhang and Jian Song

European Journal of Medicinal Chemistry, 2024, 276, 116678
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Macrocyclization strategy for improving candidate profiles in medicinal chemistry

Om Darlami, Rabin Pun, Sung-Hoon Ahn, Seok-Ho Kim and Dongyun Shin

European Journal of Medicinal Chemistry, 2024, 272, 116501
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The rise of degrader drugs

Mingxing Teng and Nathanael S. Gray

Cell Chemical Biology, 2023, 30, 864
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Amphiphilic Affibody-PROTAC conjugate Self-Assembled nanoagents for targeted cancer therapy

Wenhui Gao, Xuelin Xia, Xiaoyuan Yang, Qingrong Li, Xiaoxia Xia, Wei Huang and Deyue Yan

Chemical Engineering Journal, 2024, 495, 153437
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In Vivo Self‐Assembly of PROTACs by Bioorthogonal Chemistry for Precision Cancer Therapy

Shaowen Xie, Jingjie Zhu, Yihan Peng, Fangyi Zhan, Feiyan Zhan, Chen He, Dazhi Feng, Jia Xie, Jingyu Liu, Huajian Zhu, Hong Yao, Jinyi Xu, Zhigui Su and Shengtao Xu

Angewandte Chemie, 2025, 137
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Potent PROTACs Targeting EGFR Mutants in Drug Discovery

Robert B. Kargbo

ACS Med. Chem. Lett., 2022, 13, 1835
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Fatty acid synthase (FASN) signalome: A molecular guide for precision oncology

Javier A. Menendez, Elisabet Cuyàs, Jose Antonio Encinar, Travis Vander Steen, Sara Verdura, Àngela Llop‐Hernández, Júlia López, Eila Serrano‐Hervás, Sílvia Osuna, Begoña Martin‐Castillo and Ruth Lupu

Molecular Oncology, 2024, 18, 479
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Paired Electro‐Synthesis of Remote Amino Alcohols with/in H2O

Xinyue Fang, Xinwei Hu, Quan‐Xin Li, Shao‐Fei Ni and Zhixiong Ruan

Angewandte Chemie, 2025, 137
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Tumor‐Activated Prodrug with Synergistic Anti‐Stemness Chemical and Photodynamic Therapies

Jianhua Xiong, Xiaoyu Wang, Jaewon Kim, Jiankang Gong, Zhiqiang Mao, Jong Seung Kim and Zhihong Liu

Adv Funct Materials, 2024, 34
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BRAFV600E‐PROTAC versus inhibitors in melanoma cells: Deep transcriptomic characterization

Solomon O. Alhassan, Zakaria Y. Abd Elmageed, Youssef Errami, Guangdi Wang, Joe A. Abi‐Rached, Emad Kandil and Mourad Zerfaoui

Clinical & Translational Med, 2025, 15
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Second-Generation AUTACs for Targeted Autophagic Degradation

Daiki Takahashi, Taiichi Ora, Shigekazu Sasaki, Naoki Ishii, Toshio Tanaka, Takumi Matsuda, Mutsuki Ikeda, Jun Moriyama, Nobuo Cho, Hiroshi Nara, Hironobu Maezaki, Masahiro Kamaura, Kenichiro Shimokawa and Hirokazu Arimoto

J. Med. Chem., 2023, 66, 12342
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Proteolysis-Targeting Chimeras (PROTACs) targeting the BCR-ABL for the treatment of chronic myeloid leukemia – a patent review

André T. S. Vicente and Jorge A.R. Salvador

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Chemical Proteomics Identifies RBBP7 as a New E3 Ligase Supporting Targeted Protein Degradation

Yue Liu, Tao Yang, Lei Huang, Shengrong Li, Tongzheng Liu, Yi Tan and Zhengqiu Li

Angewandte Chemie, 2025
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PROTAC technology: From drug development to probe technology for target deconvolution

Si Yan, Guangshuai Zhang, Wei Luo, Mengwei Xu, Rui Peng, Ziwei Du, Yan Liu, Zhaofang Bai, Xiaohe Xiao and Shuanglin Qin

European Journal of Medicinal Chemistry, 2024, 276, 116725
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The Discovery of a Specific CKIP-1 Ligand for the Potential Treatment of Disuse Osteoporosis

Yange Wei, Bo Wu, Mingqiu Liu and Chun-Ping Cui

IJMS, 2024, 25, 8870
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High‐Throughput Miniaturized Synthesis of PROTAC‐Like Molecules

Ye Tian, Maximilian Seifermann, Liana Bauer, Charlotte Luchena, Janne J. Wiedmann, Stefan Schmidt, Alexander Geisel, Sergii Afonin, Julius Höpfner, Marius Brehm, Xinyong Liu, Carsten Hopf, Anna A. Popova and Pavel A. Levkin

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Discovery and characterization of potent spiro-isoxazole-based cereblon ligands with a novel binding mode

Robert Shevalev, Luca Bischof, Alexander Sapegin, Alexander Bunev, Grigor'eva Olga, Grigory Kantin, Stanislav Kalinin and Marcus D. Hartmann

European Journal of Medicinal Chemistry, 2024, 270, 116328
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Proteomics‐Based Discovery of First‐in‐Class Chemical Probes for Programmed Cell Death Protein 2 (PDCD2)

Wenzhi Ji, Woong Sub Byun, Wenchao Lu, Xijun Zhu, Katherine A. Donovan, Brendan G. Dwyer, Jianwei Che, Linjie Yuan, Xianmixinuer Abulaiti, Steven M. Corsello, Eric S. Fischer, Tinghu Zhang and Nathanael S. Gray

Angew Chem Int Ed, 2023, 62
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Sequential Azidation/Azolation of Prenylated Derivatives and a Click Reaction Enable Selective Labeling and Degradation of RAS Protein

Youfang Gan, Xiaoqian Chen, Yuanyuan Li, Yuyang Guo and Rui Wang

J. Org. Chem., 2023, 88, 10836
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PROTACS: A technology with a gold rush-like atmosphere

Yu-Wei Wang, Li Lan, Min Wang, Jin-Yang Zhang, Yu-Hui Gao, Lei Shi and Li-Ping Sun

European Journal of Medicinal Chemistry, 2023, 247, 115037
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Protein and nonprotein targets of ubiquitin modification

Fumiyo Ikeda

American Journal of Physiology-Cell Physiology, 2023, 324, C1053
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EGFR molecular degraders: preclinical successes and the road ahead

Naveen Chand Rallabandi, Dayanand Panpatil, Digvijay Gahtory, Umashanker Navik and Raj Kumar

Future Medicinal Chemistry, 2025, 17, 633
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Discovery of Novel PDEδ Autophagic Degraders: A Case Study of Autophagy-Tethering Compound (ATTEC)

Jingying Bao, Zhenqian Chen, Yu Li, Long Chen, Wei Wang, Chunquan Sheng and Guoqiang Dong

ACS Med. Chem. Lett., 2024, 15, 29
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Epigenetic therapy meets targeted protein degradation: HDAC-PROTACs in cancer treatment

Md Sadique Hussain, Liming Zhang, Amita Joshi Rana, Mudasir Maqbool, Sumel Ashique, Yumna Khan, Vikas Jakhmola, Ali Hanbashi, Wedad Mawkili and Gyas Khan

Future Medicinal Chemistry, 2025, 17, 1725
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Methods to accelerate PROTAC drug discovery

Jeyan Osman, Philip E. Thompson, Manuela Jörg and Martin J. Scanlon

Biochemical Journal, 2025, 482, 921
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Cutting-edge biotherapeutics and advanced delivery strategies for the treatment of metabolic dysfunction-associated steatotic liver disease spectrum

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Journal of Controlled Release, 2025, 380, 433
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Unraveling the secrets of novel PROTACs to improve degradation efficacy

Juan Huang, Xiaoyan Yang, Qiuqian Huang, Yangyang Gao, Pradeepa C. G. Bandaranayake, Wishwajith Kandegama, Charles R. Ashby, Yawen Dong, Zhenchao Wang and Ge-Fei Hao

Mol Divers, 2025
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Design of Murine Double Minute 2 Proteolysis Targeting Chimera Degraders with a Built-In Tumor-Targeting Ability

Zhuqian Wang, Siran Yue, Xinxin Chen, Jin Li, Peixi Zhu, Hongzhen Chen, Fang Qiu, Duoli Xie, Yiying Liang, Defang Li, Aiping Lu and Chao Liang

J. Med. Chem., 2024, 67, 18865
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O-GlcNAcylation stabilized WTAP promotes GBM malignant progression in an N6-methyladenosine-dependent manner

Jiawei Qiu, Rongrong Zhao, Caizhi Ma, Qingtong Wang, Boyan Li, Yanhua Qi, Ziwen Pan, Shulin Zhao, Shaobo Wang, Zijie Gao, Xiaofan Guo, Wei Qiu, Weijie Tang, Xing Guo, Lin Deng, Hao Xue and Gang Li

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Acceleration of Protein Degradation by 20S Proteasome-Binding Peptides Generated by In Vitro Artificial Evolution

Yunhao Zhu, Kaishin Shigeyoshi, Yumiko Hayakawa, Sae Fujiwara, Masamichi Kishida, Hitoshi Ohki, Tomohisa Horibe, Masafumi Shionyu, Tamio Mizukami and Makoto Hasegawa

IJMS, 2023, 24, 17486
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Proteolysis Targeting Chimeras (PROTACs) based on celastrol induce multiple protein degradation for triple-negative breast cancer treatment

Xuelan Gan, Fan Wang, Jianguo Luo, Yunfei Zhao, Yan Wang, Chao Yu and Jun Chen

European Journal of Pharmaceutical Sciences, 2024, 192, 106624
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New techniques and strategies in drug discovery (2020–2024 update)

Qijie Gong, Jian Song, Yihui Song, Kai Tang, Panpan Yang, Xiao Wang, Min Zhao, Liang Ouyang, Li Rao, Bin Yu, Peng Zhan, Saiyang Zhang and Xiaojin Zhang

Chinese Chemical Letters, 2025, 36, 110456
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Precise HER2 Protein Degradation via Peptide‐Conjugated Photodynamic Therapy for Enhanced Breast Cancer Immunotherapy

Changyong Guo, Fei Gao, Guoyuan Wu, Jinqiu Li, Chunquan Sheng, Shipeng He and Honggang Hu

Advanced Science, 2025, 12
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The application of PROTAC in HDAC

Shaoting Chen, Yuxiang Zheng, Benji Liang, Yudong Yin, Jian Yao, Quande Wang, Yanghan Liu and Nouri Neamati

European Journal of Medicinal Chemistry, 2023, 260, 115746
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Enhanced cellular therapy: revolutionizing adoptive cellular therapy

Meng-Yao Xu, Na Zeng, Chen-Qian Liu, Jian-Xuan Sun, Ye An, Si-Han Zhang, Jin-Zhou Xu, Xing-Yu Zhong, Si-Yang Ma, Hao-Dong He, Jia Hu, Qi-Dong Xia and Shao-Gang Wang

Exp Hematol Oncol, 2024, 13
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Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation

Martin P. Schwalm, Amelie Menge, Lewis Elson, Francesco A. Greco, Matthew B. Robers, Susanne Müller and Stefan Knapp

ACS Chem. Biol., 2025, 20, 94
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Recent advances in the molecular design and applications of proteolysis targeting chimera-based multi-specific antiviral modality

Yang Zhou, Shujing Xu, Nerea López-Carrobles, Dang Ding, Xinyong Liu, Luis Menéndez-Arias and Peng Zhan

Acta Materia Medica, 2023, 2
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Strategies for Precise Modulation of Protein Degradation

Shipeng He, Guoqiang Dong and Chunquan Sheng

Acc. Chem. Res., 2025, 58, 1236
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Identification of potent and orally bioavailable GSPT1 molecular glue degraders

Run-Duo Gao, Wenzhong Liu, Yuanyuan Liu, Grace Xie, Haotian Fang, Xingxing Xu, Meilu Yan and Shu-Li You

Bioorganic & Medicinal Chemistry Letters, 2025, 129, 130375
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Targeting METTL3 protein by proteolysis-targeting chimeras: A novel therapeutic approach for acute myeloid leukemia

Rukiye Nar, Zhixing Wu, Yafang Li, Alexis Smith, Yutao Zhang, Jue Wang, Fang Yu, Sanhui Gao, Chunjie Yu, Zhiguang Huo, Guangrong Zheng and Zhijian Qian

Genes & Diseases, 2025, 12, 101452
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The design, synthesis and bioactivity evaluation of novel androgen receptor degraders based on hydrophobic tagging

Ying Sun, Huating Wang, Yaru Li, Zhaoxiang Li, Zhihui Mao, Mengyao Zhang, Yixian Shao, Jiaqi Ye, Dan Li and Lihong Shan

Bioorganic Chemistry, 2024, 146, 107309
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Photo-Activated PROTACs for Targeted BRD4 Degradation and Synergistic Photodynamic Therapy in Bladder Cancer

Ke Wang, Mingzhu Zhang, Cheng Huang, Jishuang Zhang, Yinan Hua, Xinlu Qin, Yongming Deng, Shaohua Wei and Lin Zhou

Mol. Pharmaceutics, 2025, 22, 3388
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DNA-based nanostructures for cell membrane receptor regulation and disease treatment

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What is the future of click chemistry in drug discovery and development?

Ana C. Amorim and Anthony J. Burke

Expert Opinion on Drug Discovery, 2024, 19, 267
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Development of PROTACs using computational approaches

Jingxuan Ge, Chang-Yu Hsieh, Meijing Fang, Huiyong Sun and Tingjun Hou

Trends in Pharmacological Sciences, 2024, 45, 1162
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POT, an optogenetics-based endogenous protein degradation system

Yunyue Chen, Siyifei Wang, Luhao Zhang, Dandan Peng, Ke Huang, Baohua Ji, Junfen Fu and Yingke Xu

Commun Biol, 2025, 8
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A Dual-Targeted Molecule for Disease-Activatable Proteolysis Targeting Chimeras and Targeted Radionuclide Therapy of Cancer

Yuan Zhang, Wei Gu, Wan Chen, Jieli Zhu, Longfei Fan, Liwen Zhang, Liangyou Zhao and Qingqing Miao

J. Am. Chem. Soc., 2025, 147, 7897
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Development of Ligands and Degraders Targeting MAGE-A3

Ke Li, Mackenzie W. Krone, Arseniy Butrin, Michael J. Bond, Brian M. Linhares and Craig M. Crews

J. Am. Chem. Soc., 2024, 146, 24884
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Sequential responsive nano-PROTACs for precise intracellular delivery and enhanced degradation efficacy in colorectal cancer therapy

Liuqing Yang, Ye Yang, Jing Zhang, Minghui Li, Long Yang, Xing Wang, Meifang Chen, Hua Zhang, Bing He, Xueqing Wang, Wenbing Dai, Yiguang Wang and Qiang Zhang

Sig Transduct Target Ther, 2024, 9
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Small molecules for Kirsten rat sarcoma viral oncogene homolog mutant cancers: Past, present, and future

Peiliang Dong, Jiating Ni, Xinyue Zheng, Mingtao Wang, Meng Yang and Hua Han

European Journal of Pharmacology, 2025, 996, 177428
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NDA Submission of Vepdegestrant (ARV-471) to U.S. FDA: The Beginning of a New Era of PROTAC Degraders

Zonghui Ma and Jia Zhou

J. Med. Chem., 2025, 68, 14129
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Activation of the 26S Proteasome to Reduce Proteotoxic Stress and Improve the Efficacy of PROTACs

Jindrich Sedlacek

ACS Pharmacol. Transl. Sci., 2025, 8, 21
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Discovery of novel rigid STING PROTAC degraders as potential therapeutics for acute kidney injury

Rongxiang Ma, Renquan Fu, Yifan Wang, Kabonde Makasa Njobvu, Yapeng Fan, Zichao Yang, Mingbing Chen, Feifei Liu, Zhongping Jiang, Yong Rao, Ling Huang, Congjun Xu, Jianjun Chen and Jin Liu

European Journal of Medicinal Chemistry, 2025, 290, 117539
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Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research

Janet Caceres-Cortes, Bradley Falk, Luciano Mueller and T G Murali Dhar

J. Med. Chem., 2024, 67, 1701
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Advancing Proteolysis Targeting Chimera (PROTAC) Nanotechnology in Protein Homeostasis Reprograming for Disease Treatment

Mengyao Wu, Yilan Zhao, Chi Zhang and Kanyi Pu

ACS Nano, 2024, 18, 28502
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Exploring Degradation of Intrinsically Disordered Protein Yes-Associated Protein Induced by Proteolysis TArgeting Chimeras

Chen Zhou, Chunbao Sun, Miao Huang, Xin Tang, Liya Pi and Chenglong Li

J. Med. Chem., 2024, 67, 15168
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Development of natural product-based targeted protein degraders as anticancer agents

Cheng Chen, Yanyan Feng, Chen Zhou, Zhouyan Liu, Ziwei Tang, Ye Zhang, Tong Li, Chenglei Gu and Jichao Chen

Bioorganic Chemistry, 2024, 153, 107772
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Protein degradation: expanding the toolbox to restrain cancer drug resistance

Hui Ming, Bowen Li, Jingwen Jiang, Siyuan Qin, Edouard C. Nice, Weifeng He, Tingyuan Lang and Canhua Huang

J Hematol Oncol, 2023, 16
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Enzyme‐Activated Orthogonal Proteolysis Chimeras for Tumor Microenvironment‐Responsive Immunomodulation

Caixia Sun, Songhan Liu, Jun Wei Lau, Hanyu Yang, Yun Chen and Bengang Xing

Angewandte Chemie, 2025, 137
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Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors

Qiangfeng Wang, Yumeng Zhu and Junping Pei

Future Medicinal Chemistry, 2024, 16, 1923
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Discovery of a PROTAC degrader for METTL3-METTL14 complex

Wenhao Du, Yuting Huang, Xiaoai Chen, Yue Deng, Yaoliang Sun, Hong Yang, Qiongyu Shi, Feifei Wu, Guobin Liu, He Huang, Jian Ding, Xun Huang and Shilin Xu

Cell Chemical Biology, 2024, 31, 177
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Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity

Jenny Desantis, Alessandro Bazzacco, Michela Eleuteri, Sara Tuci, Elisa Bianconi, Antonio Macchiarulo, Beatrice Mercorelli, Arianna Loregian and Laura Goracci

European Journal of Medicinal Chemistry, 2024, 268, 116202
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Molecular Glue Discovery: Current and Future Approaches

Jeffrey A. Dewey, Clémence Delalande, Saara-Anne Azizi, Vivian Lu, Dionysios Antonopoulos and Gyorgy Babnigg

J. Med. Chem., 2023, 66, 9278
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Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus infection

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European Journal of Medicinal Chemistry, 2024, 264, 115979
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Discovery of a miniaturized PROTAC with potent activity and high selectivity

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Targeted Extracellular Protein Degradation by Dendronized DNA Chimeras

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ACS Chem. Biol., 2024, 19, 654
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Unraveling the Engagement of Kinases to CRBN Through a Shared Structural Motif to Optimize PROTACs Efficacy

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Biomolecules, 2025, 15, 206
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Proteolysis‐targeting chimeras in antiviral therapy: Leveraging influenza virus and exosome‐mediated delivery for targeted protein degradation and therapeutic advancements

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Proximity-dependent protein (de)stabilization: screening the human ORFeome for protein degraders and stabilizers

Thomas Hermanns and Kay Hofmann

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Enhancing therapeutic efficacy in homologous recombination-proficient pancreatic cancer via the combination of PARP1-PROTAC and a BRD4 inhibitor

Chunlan Pu, Yuanyuan Liu, Suke Lan, Hengrui Fan, Lvye Liu, Jianyu Liu and Yuanbiao Guo

Bioorganic & Medicinal Chemistry, 2024, 115, 117970
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Covalent Proximity Inducers

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Identification and structural basis of C-terminal cyclic imides as natural degrons for cereblon

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Refining treatment strategies for non-small cell lung cancer lacking actionable mutations: insights from multi-omics studies

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N-Degron PROTACs as a Potential Therapeutic Approach for Chronic Myeloid Leukemia

Grace Hohman and Mohamed A. Eldeeb

ACAMC, 2025, 25, 813
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Non-coding RNA and drug resistance in head and neck cancer

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Targeting Ras with protein engineering

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Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: Past, present and future perspectives

Si Ha, Jiacheng Zhu, Hua Xiang and Guoshun Luo

Chinese Chemical Letters, 2024, 35, 109192
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RIPTACs: A groundbreaking approach to drug discovery

Zonghui Ma, Andrew A. Bolinger and Jia Zhou

Drug Discovery Today, 2023, 28, 103774
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Self‐Oxygenating PROTAC Microneedle for Spatiotemporally‐Confined Protein Degradation and Enhanced Glioblastoma Therapy

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A Tumor-Specific Membrane Protein Degradation Platform via Covalent Reaction-Induced Aggregation

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ACS Appl. Mater. Interfaces, 2025, 17, 46667
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Chemically synthesized phosphorylated ubiquitin unlocks parkin for activation-controlled PROTAC platforms

Fangdan Chen, Qing Zhan, Qian Qu, Siyi Cui, Yicheng Weng, Man Pan, Qingyun Zheng, Honggang Hu and Yuanyuan Yu

Sci. China Chem., 2025
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Proteolysis Targeting Chimera Degraders of the METTL3–14 m6A-RNA Methyltransferase

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JACS Au, 2024, 4, 713
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The Quest for Oral PROTAC drugs: Evaluating the Weaknesses of the Screening Pipeline

Giulia Apprato, Giuseppe Ermondi and Giulia Caron

ACS Med. Chem. Lett., 2023, 14, 879
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X‐ray controlled release strategy in cancer therapy

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BMEMat, 2025
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PROTAC Delivery Strategies for Overcoming Physicochemical Properties and Physiological Barriers in Targeted Protein Degradation

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Pharmaceutics, 2025, 17, 501
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Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications

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J. Med. Chem., 2024, 67, 5185
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Methylarginine targeting chimeras for lysosomal degradation of intracellular proteins

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Prediction of Proteolysis-Targeting Chimeras Retention Time Using XGBoost Model Incorporated with Chromatographic Conditions

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J. Chem. Inf. Model., 2025, 65, 613
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PROTACs in the Management of Prostate Cancer

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Molecules, 2023, 28, 3698
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PROTAC Prodrug‐Integrated Nanosensitizer for Potentiating Radiation Therapy of Cancer

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Targeted protein posttranslational modifications by chemically induced proximity for cancer therapy

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Journal of Biological Chemistry, 2023, 299, 104572
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Could Targeting NPM1c+ Misfolding Be a Promising Strategy for Combating Acute Myeloid Leukemia?

Daniele Florio and Daniela Marasco

IJMS, 2024, 25, 811
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Unleashing the Power of Covalent Drugs for Protein Degradation

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Medicinal Research Reviews, 2025, 45, 1045
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Recent advances in medicinal chemistry strategies for the development of METTL3 inhibitors

Gengwu Li, Wei Chen, Dan Liu and Shibing Tang

European Journal of Medicinal Chemistry, 2025, 290, 117560
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Acetyl-CoA Carboxylase Proteolysis-Targeting Chimeras: Conceptual Design and Application as Insecticides

Qi Xu, Hao Feng, Zhong Li and Xusheng Shao

J. Agric. Food Chem., 2024, 72, 18809
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Microorganism‐Derived Bisindole Alkaloids With Anticancer Potential and Their Mechanisms: A Comprehensive Review

Zi‐Long Zhang, Hao‐Nan Xu, Chuan‐Ming Gong, Yu‐Ze Li, Xiao‐Mei Song, Yi‐Ming Li, Dong‐Dong Zhang and Rui Wang

Chemistry & Biodiversity, 2025, 22
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Targeted protein degradation in cancers: Orthodox PROTACs and beyond

Jin Li, Xinxin Chen, Aiping Lu and Chao Liang

The Innovation, 2023, 4, 100413
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Orally Bioavailable Proteolysis-Targeting Chimeras: An Innovative Approach in the Golden Era of Discovering Small-Molecule Cancer Drugs

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Expanding the ligand spaces for E3 ligases for the design of protein degraders

Rahman Shah Zaib Saleem, Martin P. Schwalm and Stefan Knapp

Bioorganic & Medicinal Chemistry, 2024, 105, 117718
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Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo

Xudong Pang, Dawei Cui, Binhua Lv and Cheng-Yun Wang

J. Med. Chem., 2024, 67, 1563
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X‐Ray‐Induced Drug Release for Cancer Therapy

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Angew Chem Int Ed, 2023, 62
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EGFR Targeted Liposomal PROTAC Assisted With Epigenetic Regulation as an Efficient Strategy for Osimertinib‐Resistant Lung Cancer Therapy

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Advanced Science, 2025
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Drugging Protein Tyrosine Phosphatases through Targeted Protein Degradation

Jinmin Miao and Zhong‐Yin Zhang

ChemMedChem, 2024, 19
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