Zhe Zhuang, Woong Sub Byun, Jakub Chrustowicz, Zuzanna Kozicka, Veronica L. Li, Dinah M. Abeja, Katherine A. Donovan, Sara Sepic, Inchul You, Mikołaj Słabicki, Eric S. Fischer, Stephen M. Hinshaw, Benjamin L. Ebert, Brenda A. Schulman and Nathanael S. Gray

Nat Chem Biol, 2026
DOI: 10.1038/s41589-026-02182-5

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

Martin P. Schwalm, Krishna Saxena, Susanne Müller and Stefan Knapp

Nat Protoc, 2024, 19, 2317
DOI: 10.1038/s41596-024-00979-z

Screening for molecular glues – Challenges and opportunities

Geoffrey A. Holdgate, Catherine Bardelle, Sophia K. Berry, Alice Lanne and Maria Emanuela Cuomo

SLAS Discovery, 2024, 29, 100136
DOI: 10.1016/j.slasd.2023.12.008

Restoring adapter protein complex 4 function with small molecules: an in silico approach to spastic paraplegia 50

Serena Francisco, Lorenzo Lamacchia, Attilio Turco, Giuseppe Ermondi, Giulia Caron and Matteo Rossi Sebastiano

Protein Science, 2025, 34
DOI: 10.1002/pro.70006

Strengths, Weaknesses, Opportunities, and Potential Threat Analysis of Targeting Leucine-Rich Repeat Kinase 2 for Parkinson’s Disease Treatment: Status Quo and Quo Vadis

Chenyu Dang, Zifan Feng, Tao Xu, Mi Li, Zhipeng Wang, Hualong Song and Ru-Bing Wang

J. Med. Chem., 2025, 68, 13148
DOI: 10.1021/acs.jmedchem.5c00013

The 17th EFMC Short Course on Medicinal Chemistry on Small Molecule Protein Degraders

Alessio Ciulli, Suzanne O'Connor, Chun‐Wa Chung, Ingo V. Hartung, Andrea Testa, Danette L. Daniels and Laura H. Heitman

ChemMedChem, 2023, 18
DOI: 10.1002/cmdc.202300464

Machine learning in targeted protein degradation drug design: a technical review of PROTACs and molecular glues

Chieh-Te Lin, Ya-Ping Shiau and Chu-Chung Lin

Drug Discovery Today, 2026, 31, 104563
DOI: 10.1016/j.drudis.2025.104563

Computational approaches enhance the design of molecular glue degraders for undruggable proteins

Sirishantha G.M.A. Deshani, Gunarathna R.D.S. Madushani, Karunaratne Veranja, Kumar Vinit and Hao Ge-Fei

Drug Discovery Today, 2026, 31, 104577
DOI: 10.1016/j.drudis.2025.104577

Elaboration of molecular glues that target TRIM21 into TRIMTACs that degrade protein aggregates

Marc A. Scemama de Gialluly, Anthony R. Allen, Elijah H. Hayes, Patrick Zhuang, Ralston B. Goldfarb, Amanda N. Farrar, Yuriy Fedorov and Drew J. Adams

Nat Commun, 2025, 16
DOI: 10.1038/s41467-025-61818-7

Targeted protein degradation of Wnt/β-catenin signaling pathway: an effective strategy for cancer therapy

Shuyang Mao, Xiaofan Zhang, Yijun Zhao, Xingxing Li, Zitong Wang, Pan Zhou, Zixuan Wang, Xiaofei Zhang, Xiamin Hu, Gang Huang and Wei Xie

J Transl Med, 2025, 23
DOI: 10.1186/s12967-025-07333-1

Identification of a Novel Substrate for eEF2K and the AURKA‐SOX8 as the Related Pathway in TNBC

Xiaoya Wan, Rong Gong, Xiaobao Zhao, Yizhi Li, Tianjiao Shan, Changxin Zhong, Rongfeng Zhu, Zonglin Chen, Shilong Jiang, Linhao He, Shijun Cao, Sheng Tian, Jinming Yang, Na Ye, Wenjun Yi and Yan Cheng

Advanced Science, 2025, 12
DOI: 10.1002/advs.202412985

Microproteins: novel multi-functional regulators in health and disease

Jiapeng He, Haozhe Zhang, Bin Liao, Qianyu Xu, Jeremy Yuen-Chun Teoh, Chi-Fai Ng, Dinglan Wu, Xian-Tao Zeng, Chris Soon Heng Tan and Hailiang Hu

Oral Science and Homeostatic Medicine, 2025, 1, 9610036
DOI: 10.26599/OSHM.2025.9610036

Enhancing protein interactions in Zein-β-lactoglobulin complexes by (-)-Epigallocatechin-3-gallate: Expanding the potential of molecular glues in food application

Qingbo Jiao, Gerui Ren, Nan Lv, Hao Li, Tianrong Wang, Min Huang, Ruibo Wu, Zexing Cao and Hujun Xie

Food Hydrocolloids, 2025, 167, 111398
DOI: 10.1016/j.foodhyd.2025.111398

Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy

Xin Han and Yi Sun

Cell Reports Physical Science, 2022, 3, 101062
DOI: 10.1016/j.xcrp.2022.101062

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
DOI: 10.1186/s13045-023-01398-5

Biophysical and Computational Approaches to Study Ternary Complexes: A ‘Cooperative Relationship’ to Rationalize Targeted Protein Degradation

Jake A. Ward, Carles Perez‐Lopez and Cristina Mayor‐Ruiz

ChemBioChem, 2023, 24
DOI: 10.1002/cbic.202300163

Discovery of a molecular glue for EGFR degradation

Hairui Wang, Hui Wang, Rui Wang, Yuanzhen Li, Zhipeng Wang, Wenshen Zhou, Li Deng, Xiyin Li, Li Zou, Qin Yang, Ren Lai, Xiaowei Qi, Jianyun Nie and Baowei Jiao

Oncogene, 2025, 44, 545
DOI: 10.1038/s41388-024-03241-8

Therapeutic targeting of CDK12: a medicinal chemistry perspective

Feifei Wang, Hongxue Dai, Kuanxin Wan and Mingliang Wang

Bioorganic & Medicinal Chemistry, 2026, 135, 118552
DOI: 10.1016/j.bmc.2026.118552

Rational engineering of degradation tail-driven CELMoD–antibody conjugates for precision malignancy therapy

Yu Guo, Yi Song, Hanlin Wang, Yang Lu, Jingyu Zhang, Zheyuan Shen, Weijuan Kan, Yuxian Wang, Haiting Duan, Shuangshuang Geng, Bo Wang, Shaoting Li, Bizhi Li, Xi Chen, Shanshan Pei, Luo Fang, Jia Li, Yubo Zhou, Jinxin Che and Xiaowu Dong

Acta Pharmaceutica Sinica B, 2025, 15, 6510
DOI: 10.1016/j.apsb.2025.09.009

Kinase-Bench: Comprehensive Benchmarking Tools and Guidance for Achieving Selectivity in Kinase Drug Discovery

Tian-Hua Wei, Shuang-Shuang Zhou, Xiao-Long Jing, Jia-Chuan Liu, Meng Sun, Zong-Hao Zhao, Qing-Qing Li, Zi-Xuan Wang, Jin Yang, Yun Zhou, Xue Wang, Cheng-Xiao Ling, Ning Ding, Xin Xue, Yan-Cheng Yu, Xiao-Long Wang, Xiao-Ying Yin, Shan-Liang Sun, Peng Cao, Nian-Guang Li and Zhi-Hao Shi

J. Chem. Inf. Model., 2024, 64, 9528
DOI: 10.1021/acs.jcim.4c01830

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
DOI: 10.1021/acs.jmedchem.3c00449

Targeted protein degradation with small molecules for cancer immunotherapy

Zichao Yang, Jianwei Xu, Xixiang Yang and Jianjun Chen

Asian Journal of Pharmaceutical Sciences, 2025, 20, 101058
DOI: 10.1016/j.ajps.2025.101058

Valorization of residual lignin from corncob residues into thermosensitive lignin-based “molecular glues” for recycling cellulase

Jinxian Shan, Feiyun Li, Hongming Lou and Yanjun Tang

International Journal of Biological Macromolecules, 2024, 279, 135474
DOI: 10.1016/j.ijbiomac.2024.135474

Rational Proteolysis Targeting Chimera Design Driven by Molecular Modeling and Machine Learning

Shuoyan Tan, Zhenglu Chen, Ruiqiang Lu, Huanxiang Liu and Xiaojun Yao

WIREs Comput Mol Sci, 2025, 15
DOI: 10.1002/wcms.70013

The antitumor peptide M1-20 induced the degradation of CDK1 through CUL4-DDB1-DCAF1-involved ubiquitination

Huitong Bu, Chaozhu Pei, Min Ouyang, Yan Chen, Li Yu, Xiaoqin Huang and Yongjun Tan

Cancer Gene Ther, 2025, 32, 61
DOI: 10.1038/s41417-024-00855-8

Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity

Yaoguang Huang, Wenwu Liu, Changhao Zhao, Xiaoyu Shi, Qingchun Zhao, Jingming Jia and Anhua Wang

European Journal of Medicinal Chemistry, 2024, 275, 116547
DOI: 10.1016/j.ejmech.2024.116547

Development and therapeutic potential of GSPT1 molecular glue degraders: A medicinal chemistry perspective

Xiujin Chang, Fangui Qu, Chunxiao Li, Jingtian Zhang, Yanqing Zhang, Yuanyuan Xie, Zhongpeng Fan, Jinlei Bian, Jubo Wang, Zhiyu Li and Xi Xu

Medicinal Research Reviews, 2024, 44, 1727
DOI: 10.1002/med.22024

Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies

Xiaopeng Peng, Zhihao Hu, Limei Zeng, Meizhu Zhang, Congcong Xu, Benyan Lu, Chengpeng Tao, Weiming Chen, Wen Hou, Kui Cheng, Huichang Bi, Wanyi Pan and Jianjun Chen

Acta Pharmaceutica Sinica B, 2024, 14, 533
DOI: 10.1016/j.apsb.2023.09.003

Discovery of a Drug-like, Natural Product-Inspired DCAF11 Ligand Chemotype

Gang Xue, Jianing Xie, Matthias Hinterndorfer, Marko Cigler, Lara Dötsch, Hana Imrichova, Philipp Lampe, Xiufen Cheng, Soheila Rezaei Adariani, Georg E. Winter and Herbert Waldmann

Nat Commun, 2023, 14
DOI: 10.1038/s41467-023-43657-6

Crbn-based molecular Glues: Breakthroughs and perspectives

Juzeng An and Xiaojun Zhang

Bioorganic & Medicinal Chemistry, 2024, 104, 117683
DOI: 10.1016/j.bmc.2024.117683

Benchmarking Cofolding Methods for Molecular Glue Ternary Structure Prediction

Yiyan Liao, Jintao Zhu, Juan Xie, Luhua Lai and Jianfeng Pei

J. Chem. Inf. Model., 2025, 65, 11136
DOI: 10.1021/acs.jcim.5c01860

Electrophile Determines Cellular Phenotypes among XPO1-Targeting Small Molecules

Yi Fan Chen, Yanqiu Shen, David F. Yan, Maryam Ghazala, Marc A. Scemama de Gialluly, Ramya Srinivasan, Amanda N. Farrar, Ryan M. Friedrich and Drew J. Adams

J. Med. Chem., 2024, 67, 12033
DOI: 10.1021/acs.jmedchem.4c00754

Broad Target Screening Reveals Abundance of FKBP12-Based Molecular Glues in Focused Libraries

Johannes K. Dreizler, Christian Meyners, Wisely Oki Sugiarto, Maximilian L. Repity, Edvaldo V. S. Maciel, Patrick L. Purder, Frederik Lermyte, Stefan Knapp and Felix Hausch

J. Med. Chem., 2025, 68, 9525
DOI: 10.1021/acs.jmedchem.5c00220

Research progress in small-molecule modulators of protein-protein interactions

Bin Yang and Xiangbing Qi

Chin. Sci. Bull., 2023, 68, 3005
DOI: 10.1360/TB-2023-0034

A Novel Paradigm for Targeting Challenging Targets: Advancing Technologies and Future Directions of Molecular Glue Degraders

Yifan Zhang, Linlin Li, Jiajia Xu, Chunchen Che, Jiaqing Jia, Haohao Lu, Qidong You and Xiaoli Xu

Molecules, 2026, 31, 459
DOI: 10.3390/molecules31030459

Proximity-Induced Pharmacology for Amyloid-Related Diseases

Andrea Bertran-Mostazo, Gabrielė Putriūtė, Irene Álvarez-Berbel, Maria Busquets, Carles Galdeano, Alba Espargaró and Raimon Sabate

Cells, 2024, 13, 449
DOI: 10.3390/cells13050449

Sculponeatin A promotes the ETS1-SYVN1 interaction to induce SLC7A11/xCT-dependent ferroptosis in breast cancer

Peng Peng, Yuliang Ren, Fang Wan, Miao Tan, Hui Wu, Jie Shen, Chen Qian, Xuewen Liu, Yuchen Xiang, Qingqing Yu, Liang Zhang, Yuan Si and Ying Liu

Phytomedicine, 2023, 117, 154921
DOI: 10.1016/j.phymed.2023.154921

Molecular Glue-Design-Evaluator (MOLDE): An Advanced Method for In-Silico Molecular Glue Design

A. S. Ben Geoffrey, Deepak Agrawal, Nagaraj M. Kulkarni and Manonmani Gunasekaran

ACS Omega, 2025, 10, 6650
DOI: 10.1021/acsomega.4c08049

Progress on molecular glue degraders

Jiaqi Chen, Zhiheng Deng, Haoxiang Li and Lei Liu

Sci. Sin.-Chim, 2026
DOI: 10.1360/SSC-2025-0228

Chemical and genetic molecular glues to degrade CoREST corepressors

Ying-Qi Song, Qingjun Li and Chunquan Sheng

Acta Pharmaceutica Sinica B, 2025, 15, 4964
DOI: 10.1016/j.apsb.2025.07.006

From intuition to AI: evolution of small molecule representations in drug discovery

Miles McGibbon, Steven Shave, Jie Dong, Yumiao Gao, Douglas R Houston, Jiancong Xie, Yuedong Yang, Philippe Schwaller and Vincent Blay

Briefings in Bioinformatics, 2023, 25
DOI: 10.1093/bib/bbad422

Discovery of novel protein degraders based on bioorthogonal reaction-driven intracellular self-assembly strategy

Ru Si, Huanjie Zhu, Jin Wang, Qingqing Zhang, Yanchen Li, Xiaoyan Pan and Jie Zhang

Bioorganic Chemistry, 2023, 135, 106497
DOI: 10.1016/j.bioorg.2023.106497

Design and Discovery of Preclinical Candidate LYG-409 as a Highly Potent and Selective GSPT1 Molecular Glue Degraders

Yanqing Zhang, Wenjing Liu, Chao Tong, Xinhong Wang, Xiujin Chang, Fangui Qu, Zhiming Zhang, Zhongpen Fan, Monong Zhao, Cheng Tang, Beichen Song, Ming Ding, Zhixia Qiu, Jubo Wang, Jinlei Bian, Zhiyu Li, Hongxi Wu and Xi Xu

J. Med. Chem., 2025, 68, 2608
DOI: 10.1021/acs.jmedchem.4c01787

Discovery of fluorescent theranostic molecular glues for real-time visualization and target degradation toward eEF2K

Tingting Liu, Jie Ma, Gaopan Dong, Mei Zhang, Subin Song, Xuerui Zhang, Shixiang Qi, Mingyu Cheng, Wenjie Liu, Xu Wang and Yuqi Gao

European Journal of Medicinal Chemistry, 2026, 301, 118180
DOI: 10.1016/j.ejmech.2025.118180

From serendipity to strategy: molecular glue degraders in cancer therapeutics

Sarah Darling, Ilirjana Bajrami and Stephen C. West

Critical Reviews in Biochemistry and Molecular Biology, 2025, 60, 200
DOI: 10.1080/10409238.2025.2564068

Expanding the druggable proteome strategies and innovations in targeted protein degradation

Ke Ma, Ting Liu, Wen-Bo Huan, Ke-Zheng Chen and Sheng-Lin Qiao

Nano Today, 2026, 67, 102945
DOI: 10.1016/j.nantod.2025.102945

Accommodating Statistical and Physics-Based Computational Protocols for Molecular Glue Model and Evaluation

Qixuan Xu, Wenlang Liu, Hao Liu and Zheng Zheng

J. Chem. Inf. Model., 2025, 65, 6166
DOI: 10.1021/acs.jcim.5c00387

Protein degraders - from thalidomide to new PROTACs

Takumi Ito

The Journal of Biochemistry, 2024, 175, 507
DOI: 10.1093/jb/mvad113

Optimization and Evaluation of Complementary Degrader Discovery Assays for Application in Screening

Johanna Huchting, Arjen Weller, Moyra Schweizer, Mona Brandt, Jan Heering, Maria Kuzikov, Markus Wolf, Jeanette Reinshagen, Markus A. Queisser, Philip Gribbon, Andrea Zaliani, Ole Pless and Aimo Kannt

ACS Pharmacol. Transl. Sci., 2025, 8, 2600
DOI: 10.1021/acsptsci.5c00195

Chemical rewiring of ubiquitination by degraders and their selectivity routes

Rory Whelan and Cristina Mayor-Ruiz

Nat Struct Mol Biol, 2024, 31, 205
DOI: 10.1038/s41594-024-01215-8

CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications

Riya Thapa, Asif Ahmad Bhat, Gaurav Gupta, S. Renuka Jyothi, Irwanjot Kaur, Sachin Kumar, Naveen Sharma, G. V. Siva Prasad, Atreyi Pramanik and Haider Ali

Chem Biol Drug Des, 2024, 104
DOI: 10.1111/cbdd.70009

Development of FBXO22 Degraders and the Recruitment Ligand 2-Pyridinecarboxyaldehyde (2-PCA)

Tian Qiu, Zhe Zhuang, Woong Sub Byun, Zuzanna Kozicka, Kheewoong Baek, Jianing Zhong, Abby M. Thornhill, Julia K. Ryan, Katherine A. Donovan, Eric S. Fischer, Benjamin L. Ebert and Nathanael S. Gray

J. Am. Chem. Soc., 2025, 147, 45132
DOI: 10.1021/jacs.5c14141

Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders

Yiying Wei, Xinxin Xu, Minchuan Jiang, Yongxing Wang, Yang Zhou, Zhen Wang, Zhang Zhang, Fengtao Zhou and Ke Ding

European Journal of Medicinal Chemistry, 2023, 258, 115580
DOI: 10.1016/j.ejmech.2023.115580

Research advancements in molecular glues derived from natural product scaffolds: Chemistry, targets, and molecular mechanisms

Lina Yin, Tingting Niu, Ling Li, Wei Yu, Bo Han, Asma Rehman and Kewu Zeng

Chinese Herbal Medicines, 2025, 17, 235
DOI: 10.1016/j.chmed.2025.01.001

A platform for the rapid synthesis of molecular glues (Rapid-Glue) under miniaturized conditions for direct biological screening

Jingyao Li, Chunrong Li, Zhongrui Zhang, Zhen Zhang, Zhiping Wu, Junzhuo Liao, Zhen Wang, Meghan McReynolds, Haibo Xie, Le Guo, Qiuhua Fan, Junmin Peng and Weiping Tang

European Journal of Medicinal Chemistry, 2023, 258, 115567
DOI: 10.1016/j.ejmech.2023.115567

Oligomeric Remodeling by Molecular Glues Revealed Using Native Mass Spectrometry and Mass Photometry

Xiaojing Huang, Hari Kamadurai, Piro Siuti, Ezaz Ahmed, Jack L. Bennett and William A. Donald

J. Am. Chem. Soc., 2023, 145, 14716
DOI: 10.1021/jacs.3c02655

Drug discovery by targeting the protein–protein interactions involved in autophagy

Honggang Xiang, Mi Zhou, Yan Li, Lu Zhou and Renxiao Wang

Acta Pharmaceutica Sinica B, 2023, 13, 4373
DOI: 10.1016/j.apsb.2023.07.016

A Self-Assembled Nano-Molecular Glue (Nano-mGlu) Enables GSH/H2O2-Triggered Targeted Protein Degradation in Cancer Therapy

Jie Sun, Mingxi Gu, Lvyang Peng, Jing Guo, Peng Chen, Yalei Wen, Fang Feng, Xiaojuan Chen, Tongzheng Liu, Yongheng Chen, Xiaoyun Lu, Liqian Gao, Shao Q. Yao and Peiyan Yuan

J. Am. Chem. Soc., 2025, 147, 372
DOI: 10.1021/jacs.4c11003

Mapping the global landscape of molecular glues in drug discovery: a bibliometric analysis from 2010 to 2024

Sonali Labhade, Ritesh Bhole, Pawan Karwa, Harshad Kapare and Subhashini Singh

Naunyn-Schmiedeberg's Arch Pharmacol, 2026, 399, 4321
DOI: 10.1007/s00210-025-04630-w

Advances in molecular glues: exploring chemical space and design principles for targeted protein degradation

S Hemant Kumar, Muthukumaran Venkatachalapathy, Ramesh Sistla and Vasanthanathan Poongavanam

Drug Discovery Today, 2024, 29, 104205
DOI: 10.1016/j.drudis.2024.104205

Molecular glues for protein-protein interactions: Progressing toward a new dream

Markella Konstantinidou and Michelle R. Arkin

Cell Chemical Biology, 2024, 31, 1064
DOI: 10.1016/j.chembiol.2024.04.002

Discovery and Mechanistic Elucidation of NQO1‐Bioactivatable Small Molecules That Overcome Resistance to Degraders

Bárbara M. G. Barbosa, Aikaterini Sfyaki, Sergi Rafael, Ferran José‐Duran, Joan Pous, Carolina Sánchez‐Zarzalejo, Carles Perez‐Lopez, Mar Vilanova, Marko Cigler, Marina Gay, Marta Vilaseca, Georg E. Winter, Antoni Riera and Cristina Mayor‐Ruiz

Angew Chem Int Ed, 2024, 63
DOI: 10.1002/anie.202316730

Molecular Glue Degraders Redefining Targeted Therapies From Discovery to Therapeutic Applications

Jinfeng Wen, Jingtian Yu, Wuqiang Wen and Baishan Jiang

MedComm – Oncology, 2026, 5
DOI: 10.1002/mog2.70058

Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery

Zefeng Wang, Shabnam Shaabani, Xiang Gao, Yuen Lam Dora Ng, Valeriia Sapozhnikova, Philipp Mertins, Jan Krönke and Alexander Dömling

Nat Commun, 2023, 14
DOI: 10.1038/s41467-023-43614-3

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
DOI: 10.1016/j.ejmech.2023.115950

Recent Advances in Targeted Protein Degradation Molecular Glues as Anticancer Drugs

Yulin Shen, Wen Wen, Luoyang Chen, Nan Zhang, Wei Cong and Honggang Hu

Clin Exp Pharma Physio, 2025, 52
DOI: 10.1111/1440-1681.70064

GSPT1 degraders: research progress, development strategies and challenges

Chen Liu, Hongkang Peng, Peng Chen, Yuxiang Li, Zihao Deng, Shaojie Li, Tong Yang, Ke Liu, Zhen Wang and Linyi Liu

Bioorganic & Medicinal Chemistry, 2025, 131, 118390
DOI: 10.1016/j.bmc.2025.118390

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

Peipei Jin, Zhaozheng Chen, Ju Zhang, Haowen Li, Pengfei Wei, Ziyu Wang, Qiyu Feng, Hongyang Wang, Da Han and Yanyan Miao

Acta Biomaterialia, 2025, 195, 509
DOI: 10.1016/j.actbio.2025.02.023

Thalidomide derivatives degrade BCL-2 by reprogramming the binding surface of CRBN

Jianhui Wang, Marcel Heinz, Kang Han, Varun J. Shah, Sebastian Hasselbeck, Martin P. Schwalm, Rajeshwari Rathore, Gerhard Hummer, Jun Zhou, Ivan Dikic and Xinlai Cheng

Cell Reports Physical Science, 2024, 5, 101960
DOI: 10.1016/j.xcrp.2024.101960

Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence

Miquel Duran-Frigola, Marko Cigler and Georg E. Winter

J. Am. Chem. Soc., 2023, 145, 2711
DOI: 10.1021/jacs.2c11098

A novel lncRNA GM47544 modulates triglyceride metabolism by inducing ubiquitination-dependent protein degradation of APOC3

Qianqian Xiao, Luyun Wang, Jing Wang, Man Wang, Dao Wen Wang and Hu Ding

Molecular Metabolism, 2024, 88, 102011
DOI: 10.1016/j.molmet.2024.102011

Nucleic acid-encoded antibody gene transfer-next generation of antibody therapies

Kaikai Yu, Xiao Geng, Baichuan Chen, Na Xu and Wensen Liu

Drug Delivery, 2025, 32
DOI: 10.1080/10717544.2025.2566782

P53 upregulation by USP7-engaging molecular glues

Zhaoyang Li, Ziying Wang, Chao Zhong, Hang Zhang, Rui Liu, Ping An, Zhiqiang Ma, Junmei Lu, Chengfang Pan, Zhaolin Zhang, Zhiyuan Cao, Jianyi Hu, Dong Xing, Yiyan Fei, Yu Ding and Boxun Lu

Science Bulletin, 2024, 69, 1936
DOI: 10.1016/j.scib.2024.04.017

Bioluminescence-based assays for quantifying endogenous protein interactions in live cells

Andrew L. Niles, Michael R.C. Dibble, Thomas Machleidt, Kelli Martino, Matthew R. Swiatnicki, Elizabeth H. Vu and Marie K. Schwinn

Journal of Biological Chemistry, 2025, 301, 110454
DOI: 10.1016/j.jbc.2025.110454

Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins

Gary Tin, Marko Cigler, Matthias Hinterndorfer, Kevin D. Dong, Hana Imrichova, Steven P. Gygi and Georg E. Winter

Bioorganic & Medicinal Chemistry Letters, 2024, 107, 129779
DOI: 10.1016/j.bmcl.2024.129779

C646 degrades Exportin-1 to modulate p300 chromatin occupancy and function

Yi Fan Chen, Atikur Rahman, Joel L. Sax, Matthew J. Atala Pleshinger, Ryan M. Friedrich and Drew J. Adams

Cell Chemical Biology, 2024, 31, 1363
DOI: 10.1016/j.chembiol.2024.05.016

Covalent fragment approaches targeting non-cysteine residues

Noémi Csorba, Péter Ábrányi-Balogh and György M. Keserű

Trends in Pharmacological Sciences, 2023, 44, 802
DOI: 10.1016/j.tips.2023.08.014

Phenotypic Screening for Targeted Protein Degradation: Strategies, Challenges, and Emerging Opportunities

Baoli Ding, Jiawen Hu, Binyan Shou, Li Jiang, Bo Yang, Ji Cao and Cheng-Liang Zhu

J. Med. Chem., 2025, 68, 18024
DOI: 10.1021/acs.jmedchem.5c00949

Degradation of Cyclin-Dependent Kinase: A New Weapon for Cancer Therapy

Xing Tian, Xiaojie Dai, Ye Zhong, Maosheng Cheng and Yang Liu

Pharmaceutical Fronts, 2025, 07, e275
DOI: 10.1055/a-2742-7859

Research Progress in Targeting GSPT1: Molecular Glues, Bifunctional Degraders, and Antibody-Enabled Molecular Glues for Cancer Therapy

Binbin Cheng, Yaping Wang, Yimeng Hong, Yingxing Zhou, Jianjun Chen and Chunlai Zeng

J. Med. Chem., 2025, 68, 13169
DOI: 10.1021/acs.jmedchem.5c00783

Next steps for targeted protein degradation

Mackenzie W. Krone and Craig M. Crews

Cell Chemical Biology, 2025, 32, 219
DOI: 10.1016/j.chembiol.2024.10.004

Small molecules targeting protein–protein interactions for cancer therapy

Defa Wu, Yang Li, Lang Zheng, Huan Xiao, Liang Ouyang, Guan Wang and Qiu Sun

Acta Pharmaceutica Sinica B, 2023, 13, 4060
DOI: 10.1016/j.apsb.2023.05.035

Nanoparticle-mediated targeted protein degradation (NanoTPD): Principles, rational design and mechanisms of degradation

Yunting Zhang, Keran Wang, Yixiang Yang, Tao Gong, Zhirong Zhang, Renhe Liu and Yao Fu

Nano Today, 2026, 66, 102926
DOI: 10.1016/j.nantod.2025.102926

Proteome-scale discovery of protein degradation and stabilization effectors

Juline Poirson, Hanna Cho, Akashdeep Dhillon, Shahan Haider, Ahmad Zoheyr Imrit, Mandy Hiu Yi Lam, Nader Alerasool, Jessica Lacoste, Lamisa Mizan, Cassandra Wong, Anne-Claude Gingras, Daniel Schramek and Mikko Taipale

Nature, 2024, 628, 878
DOI: 10.1038/s41586-024-07224-3

A rapid imaging-based screen for induced-proximity degraders identifies a potent degrader of oncoprotein SKP2

Yankai Chu, Shishuang Chen, Mingyang Yang, Yin Chen, Huiling Fang, Pinyu Huang, Yueru Xie, Chi Sun, Yun Chen, Baoding Zhang, Li Li, Hongchen Mu, Ding Song, Wentao Cheng, Chao Wang, Wei Jiang, Xiaolan Xu, Zhengjin He, Shuo Chen, Mingxian Liu, Jingchuan Ma, Man Yang, Jiaqi Cao, Jing Gao, Jiali Shen, Lulu Zhang, Yu Bai, Zheyi Liu, Jingyao Chen, Siqi Dai, Yi Arial Zeng, Yun Zhao, Hu Zhou, Chong Chen, Huanwei Ru, Li Tan, Ximin Chi, Fangjun Wang, Daming Gao, Moubin Lin, Xianming Deng and Hai Jiang

Nat Biotechnol, 2025
DOI: 10.1038/s41587-025-02793-8

Opportunities in proximity modulation: Bridging academia and industry

Ivan Dikic, Cristina Mayor-Ruiz, Georg E. Winter, Kerstin Koch, Alessio Ciulli and Nicolas H. Thomä

Molecular Cell, 2025, 85, 3012
DOI: 10.1016/j.molcel.2025.07.018

Molecular glue degraders: Rational design, specificity engineering, and advanced delivery

Lieen Ma, Ning Wang, Jingjing Zhu, Lingjie Wu, Shan He and Bin Zhang

Acta Pharmaceutica Sinica B, 2026
DOI: 10.1016/j.apsb.2026.02.020

Cullin-RING Ligase 4 in Cancer: Structure, Functions, and Mechanisms

Jingyi Cheng, Xin Bin and Zhangui Tang

Biochimica et Biophysica Acta (BBA) - Reviews on Cancer, 2024, 1879, 189169
DOI: 10.1016/j.bbcan.2024.189169

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
DOI: 10.1002/1878-0261.13582

The rise of degrader drugs

Mingxing Teng and Nathanael S. Gray

Cell Chemical Biology, 2023, 30, 864
DOI: 10.1016/j.chembiol.2023.06.020

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
DOI: 10.1016/j.apsb.2024.01.010

Targeting ferroptosis opens new avenues for the development of novel therapeutics

Shumin Sun, Jie Shen, Jianwei Jiang, Fudi Wang and Junxia Min

Sig Transduct Target Ther, 2023, 8
DOI: 10.1038/s41392-023-01606-1

Unveiling Innovative anti-influenza Agents Through Modern Medicinal Chemistry Approaches (2019–2023 updates)

Chuanfeng Liu, Lide Hu, Huinan Jia, Jiwei Zhang, Guanyu Dong, Edeildo Ferreira da Silva-Júnior, Xinyong Liu and Peng Zhan

Future Med. Chem., 2023, 15, 1915
DOI: 10.4155/fmc-2023-0258

Transcriptional co-activators: emerging roles in signaling pathways and potential therapeutic targets for diseases

Priyanka Dey Talukdar and Urmi Chatterji

Sig Transduct Target Ther, 2023, 8
DOI: 10.1038/s41392-023-01651-w

Marine‐Derived Molecular Glue Degraders: A New Frontier in Targeted Protein Degradation for Treatment of Multi‐Factorial Diseases

Vajagathali Mohammed, B. Haridevamuthu, Kathiravan Muthu Kumaradoss, S. Karthick Raja Namasivayam and Jesu Arockiaraj

Biotech and App Biochem, 2026, 73, 871
DOI: 10.1002/bab.70055

Molecular glues and induced proximity: An evolution of tools and discovery

Stephanie Anne Robinson, Jennifer Anne Co and Steven Mark Banik

Cell Chemical Biology, 2024, 31, 1089
DOI: 10.1016/j.chembiol.2024.04.001

USP5 deubiquitylates and stabilizes FcεRIγ to enhance IgE-induced mast cell activation and allergic inflammation

Zi-Wen Zhou, Xue-Ting Xu, Qiu-Ni Liang, Yan-Mei Zhou, Wan-Zhen Hu, Shan Liu, Yu-Xin Jiao, Shu-Chen Zhang, Kunmei Ji and Jia-Jie Chen

Sci. Signal., 2025, 18
DOI: 10.1126/scisignal.adr3411

Synthetic and Medicinal Chemistry Perspectives on Cereblon‐Binding Molecular Glue Degraders: Recent Advances and Emerging Trends

Hyuck‐Jae Won, Seung Mok Baek, Min Hoo Lee, Jae Hyeon Park, Jeong‐Won Shin, Yo‐Sep Yang, Yoon Hu Jang, Kyung‐Soo Inn and Nam‐Jung Kim

Eur J Org Chem, 2026
DOI: 10.1002/ejoc.202501208

Discovery of Kinetin in inhibiting colorectal cancer progression via enhancing PSMB1-mediated RAB34 degradation

Xuefei Jiang, Lanlan Yang, Guanxing Chen, Xingzhi Feng, Yiting Liu, Qianling Gao, Mingru Mai, Calvin Yu-Chian Chen, Shubiao Ye and Zihuan Yang

Cancer Letters, 2024, 584, 216600
DOI: 10.1016/j.canlet.2023.216600

Targeted protein degradation: advances in drug discovery and clinical practice

Guangcai Zhong, Xiaoyu Chang, Weilin Xie and Xiangxiang Zhou

Sig Transduct Target Ther, 2024, 9
DOI: 10.1038/s41392-024-02004-x

Small-Molecule Ligands Targeting Lysosome-Shuttling Receptors and the Emerging Landscape of Lysosome-Targeting Chimeras

Jingjing Yang and Heping Zhu

J. Med. Chem., 2025, 68, 18040
DOI: 10.1021/acs.jmedchem.5c01019

An Integrated Approach Combining Surface Plasmon Resonance Screening with Proteomics Enables Discovery of Natural Molecular Glue Degraders

Yueying Yang, Rui Zhu, Jing Liang, Hongwei Yan, Huadong Zhang, Jundan Tian, Rui Zhang, Xiaofen Liu, Yang Liu, Hua Li and Lixia Chen

JACS Au, 2026, 6, 483
DOI: 10.1021/jacsau.5c01404

Epigenetics-targeted drugs: current paradigms and future challenges

Wanlin Dai, Xinbo Qiao, Yuanyuan Fang, Renhao Guo, Peng Bai, Shuang Liu, Tingting Li, Yutao Jiang, Shuang Wei, Zhijing Na, Xue Xiao and Da Li

Sig Transduct Target Ther, 2024, 9
DOI: 10.1038/s41392-024-02039-0

Discovery of a Novel Series of iso-Indolinone-Based Glutarimides as Highly Efficacious and Selective IKZF2 Molecular Glue Degraders

Xuqing Zhang, Harshil Dhruv, Qiaolin Deng, Matthew Tudor, Nelisa Bechtel, Rakesh Nagilla, Larry Jolivette, Cory T. Rice, Peter Orth, Elham Behshad, Corey Strickland, Helai P. Mohammad, Longchuan Bai, Donna McEachern, Shaomeng Wang, Zhihua Sui and E. Scott Priestley

J. Med. Chem., 2025, 68, 18230
DOI: 10.1021/acs.jmedchem.5c00668

Design, synthesis and biological evaluation of novel quinazolinone derivatives as CRBN E3 ligase modulators

Linyi Liu, Renhong Sun, Haixia Liu, Chaowei Ren, Yuedong Zhou, Xing Qiu, Ying Kong, Biao Jiang and Xiaobao Yang

European Journal of Medicinal Chemistry, 2023, 247, 115016
DOI: 10.1016/j.ejmech.2022.115016

A biotin targeting chimera (BioTAC) system to map small molecule interactomes in situ

Andrew J. Tao, Jiewei Jiang, Gillian E. Gadbois, Pavitra Goyal, Bridget T. Boyle, Elizabeth J. Mumby, Samuel A. Myers, Justin G. English and Fleur M. Ferguson

Nat Commun, 2023, 14
DOI: 10.1038/s41467-023-43507-5

Confounding Factors in Targeted Degradation of Short-Lived Proteins

Vesna Vetma, Laura Casares Perez, Ján Eliaš, Andrea Stingu, Anju Kombara, Teresa Gmaschitz, Nina Braun, Tuncay Ciftci, Georg Dahmann, Emelyne Diers, Thomas Gerstberger, Peter Greb, Giorgia Kidd, Christiane Kofink, Ilaria Puoti, Valentina Spiteri, Nicole Trainor, Harald Weinstabl, Yvonne Westermaier, Claire Whitworth, Alessio Ciulli, William Farnaby, Kirsten McAulay, Aileen B. Frost, Nicola Chessum and Manfred Koegl

ACS Chem. Biol., 2024, 19, 1484
DOI: 10.1021/acschembio.4c00152

Recent advances in targeting protein degradation for tumor immunotherapy

Shuai Li, Yushan Jin, Huanhuan Wu, Hong Yuan and Jingyuan Zhao

J Hematol Oncol, 2025, 19
DOI: 10.1186/s13045-025-01765-4

Targeting epigenetic modifications in Parkinson's disease therapy

Dan Zhang, Jifa Zhang, Yuxi Wang, Guan Wang, Pan Tang, Yun Liu, Yiwen Zhang and Liang Ouyang

Medicinal Research Reviews, 2023, 43, 1748
DOI: 10.1002/med.21962

Targeted protein degradation: therapeutic potential and challenges of PROTACs and molecular glues

Sun Kim and Eui-Bae Jeung

J Biomed Transl Res, 2025, 26, 21
DOI: 10.12729/jbtr.2025.26.2.21

Targeting the Ubiquitin–Proteasome System for Cancer

Zhaoyun Liu, Jiao Lai, Ziyu Ma, Jianhua Pan, Chun Yang and Rong Fu

MedComm, 2025, 6
DOI: 10.1002/mco2.70391

Harnessing UBR5 for targeted protein degradation of key transcriptional regulators

Asad M. Taherbhoy and Danette L. Daniels

Trends in Pharmacological Sciences, 2023, 44, 758
DOI: 10.1016/j.tips.2023.09.001

Clues for glues: from serendipity to nature’s blueprints in degrader discovery

Zuzanna Kozicka

Essays in Biochemistry, 2025, 69, 379
DOI: 10.1042/EBC20253058

Proximity-Based Modalities for Biology and Medicine

Xingui Liu and Alessio Ciulli

ACS Cent. Sci., 2023, 9, 1269
DOI: 10.1021/acscentsci.3c00395

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
DOI: 10.1016/j.bioorg.2024.107309

Native mass spectrometry for proximity-inducing compounds: a new opportunity for studying chemical-induced protein modulation

Emanuele Fabbrizi, Francesco Fiorentino, Fabrizio Casano, Antonello Mai and Dante Rotili

Expert Opinion on Drug Discovery, 2025, 20, 643
DOI: 10.1080/17460441.2025.2486146

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

Discovery and Mechanistic Elucidation of NQO1‐Bioactivatable Small Molecules That Overcome Resistance to Degraders

Bárbara M. G. Barbosa, Aikaterini Sfyaki, Sergi Rafael, Ferran José‐Duran, Joan Pous, Carolina Sánchez‐Zarzalejo, Carles Perez‐Lopez, Mar Vilanova, Marko Cigler, Marina Gay, Marta Vilaseca, Georg E. Winter, Antoni Riera and Cristina Mayor‐Ruiz

Angewandte Chemie, 2024, 136
DOI: 10.1002/ange.202316730

Mode of action of a DCAF16-recruiting targeted glue that can selectively degrade BRD9

Scott J. Hughes, Wojciech J. Stec, Colin T. R. Davies, David McGarry, Alicia Williams, Marta Carrara, Ivan Del Barco Barrantes, Rebecca Harris, Anna Tasegian, Dominic D. G. Owens, Alexander Fawcett, John Hellicar, Aleksandra Azevedo, Gregor P. Meier, Andrew C. Runcie, Liliana Greger, Martin O’Rourke, Ian Churcher, Martin Pass, Giles A. Brown, Alessio Ciulli, Louise K. Modis and Andrea Testa

Nat Commun, 2025, 16
DOI: 10.1038/s41467-025-63594-w

Design principles for cyclin K molecular glue degraders

Zuzanna Kozicka, Dakota J. Suchyta, Vivian Focht, Georg Kempf, Georg Petzold, Marius Jentzsch, Charles Zou, Cristina Di Genua, Katherine A. Donovan, Seemon Coomar, Marko Cigler, Cristina Mayor-Ruiz, Jonathan L. Schmid-Burgk, Daniel Häussinger, Georg E. Winter, Eric S. Fischer, Mikołaj Słabicki, Dennis Gillingham, Benjamin L. Ebert and Nicolas H. Thomä

Nat Chem Biol, 2024, 20, 93
DOI: 10.1038/s41589-023-01409-z

Small-Molecule Modulators Targeting Coactivator-Associated Arginine Methyltransferase 1 (CARM1) as Therapeutic Agents for Cancer Treatment: Current Medicinal Chemistry Insights and Emerging Opportunities

Shuqing Li, Wanyi Pan, Chengpeng Tao, Zhihao Hu, Binbin Cheng, Jianjun Chen and Xiaopeng Peng

J. Med. Chem., 2025, 68, 5024
DOI: 10.1021/acs.jmedchem.4c02106

Toward In Silico Design of Protein–Protein Interaction Stabilizers

Jintao Zhu, Luhua Lai and Jianfeng Pei

ACS Cent. Sci., 2023, 9, 861
DOI: 10.1021/acscentsci.3c00545

Rational discovery of molecular glue degraders based on block chemistry

Junjie Wei, Wenjing Feng, Qingsong Chen, Qianbin Li and Zhuo Chen

Drug Discovery Today, 2025, 30, 104480
DOI: 10.1016/j.drudis.2025.104480

Nanotechnology‐Enabled Targeted Protein Degradation for Cancer Therapeutics

Wutong Zhao, Yongbin Jiang, Xiufen Li and Hai Wang

WIREs Nanomed Nanobiotechnol, 2024, 16
DOI: 10.1002/wnan.2020

Linker-free PROTACs efficiently induce the degradation of oncoproteins

Jianchao Zhang, Congli Chen, Xiao Chen, Kefan Liao, Fengming Li, Xiaoxiao Song, Chaowei Liu, Ming-Yuan Su, Huiyong Sun, Tingjun Hou, Chris Soon Heng Tan, Lijing Fang and Hai Rao

Nat Commun, 2025, 16
DOI: 10.1038/s41467-025-60107-7

Inhibitors to degraders: Changing paradigm in drug discovery

V. Haridas, Souvik Dutta, Akshay Munjal and Shailja Singh

iScience, 2024, 27, 109574
DOI: 10.1016/j.isci.2024.109574