Chemistries of bifunctional PROTAC degraders

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

Chem. Soc. Rev., 2022, 51, 7066
DOI: 10.1039/D2CS00220E

Capsule-based automated synthesis for the efficient assembly of PROTAC like molecules

Samuele Bordi, Tuo Jiang, Anna Konopka, Guillaume Coin, Paula L. Nichols and Benedikt M. Wanner

Digital Discovery, 2023, 2, 848
DOI: 10.1039/D3DD00027C

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
DOI: 10.1039/D2RA03761K

Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase

Yuki Murakami, Hinata Osawa, Takashi Kurohara, Yuta Yanase, Takahito Ito, Hidetomo Yokoo, Norihito Shibata, Mikihiko Naito, Kosuke Aritake and Yosuke Demizu

RSC Med. Chem., 2022, 13, 1495
DOI: 10.1039/D2MD00284A

Predicting PROTAC-mediated ternary complexes with AlphaFold3 and Boltz-1

Nils Dunlop, Francisco Erazo, Farzaneh Jalalypour and Rocío Mercado

Digital Discovery, 2025, 4, 3782
DOI: 10.1039/D5DD00300H

Methods to characterize and discover molecular degraders in cells

Zhi Lin and Christina M. Woo

Chem. Soc. Rev., 2022, 51, 7115
DOI: 10.1039/D2CS00261B

Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation

Yu Chen, Ira Tandon, William Heelan, Yixin Wang, Weiping Tang and Quanyin Hu

Chem. Soc. Rev., 2022, 51, 5330
DOI: 10.1039/D1CS00762A

Utilising the intrinsic fluorescence of pomalidomide for imaging applications

Duncan K. Brownsey, Christopher J. Gafuik, Dae-Sun Kim, Leonie O’Sullivan, Evgueni Gorobets, Samuel Krukowski, Madison Turk, Craig N. Jenne, Douglas J. Mahoney and Darren J. Derksen

Chem. Commun., 2023, 59, 14532
DOI: 10.1039/D3CC04314B

Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1

Jiazheng Guo, Fengyi Yu, Kuojun Zhang, Sheng Jiang, Xiangyu Zhang and Tianyu Wang

RSC Med. Chem., 2024, 15, 1096
DOI: 10.1039/D3MD00636K

PROTACs: past, present and future

Ke Li and Craig M. Crews

Chem. Soc. Rev., 2022, 51, 5214
DOI: 10.1039/D2CS00193D

Chasing molecular glue degraders: screening approaches

Ana Domostegui, Luis Nieto-Barrado, Carles Perez-Lopez and Cristina Mayor-Ruiz

Chem. Soc. Rev., 2022, 51, 5498
DOI: 10.1039/D2CS00197G

Nucleic-Acid-Based Targeted Degradation in Drug Discovery

Wei Wang, Shipeng He, Guoqiang Dong and Chunquan Sheng

J. Med. Chem., 2022, 65, 10217
DOI: 10.1021/acs.jmedchem.2c00875

Proteolysis Targeting Chimera Degraders of the METTL3–14 m6A-RNA Methyltransferase

Francesco Errani, Annalisa Invernizzi, Marcin Herok, Elena Bochenkova, Fiona Stamm, Ivan Corbeski, Valeria Romanucci, Giovanni Di Fabio, František Zálešák and Amedeo Caflisch

JACS Au, 2024, 4, 713
DOI: 10.1021/jacsau.4c00040

Antioxidant Natural Compounds Integrated with Targeted Protein Degradation: A Multi-Modal Strategy for Alzheimer’s Disease Therapy

Desh Deepak Singh, Dharmendra Kumar Yadav and Dongyun Shin

Antioxidants, 2025, 14, 1426
DOI: 10.3390/antiox14121426

Green Drug Discovery: Leveraging Biodiversity for Sustainable Pharmaceutical Solutions

Arshdeep Singh, Rabin Debnath, Viney Chawla and Pooja A. Chawla

Chemistry & Biodiversity, 2026, 23
DOI: 10.1002/cbdv.202500733

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
DOI: 10.1021/acs.jmedchem.2c01721

LIMK2 promotes melanoma tumor growth and metastasis through G3BP1-ESM1 pathway-mediated apoptosis inhibition

Parmanand Malvi, Dhana Sekhar Reddy, Raj Kumar, Suresh Chava, Sneha Burela, Keshab Parajuli, Xuchen Zhang and Narendra Wajapeyee

Oncogene, 2023, 42, 1478
DOI: 10.1038/s41388-023-02658-x

Harmony of Protein Tags and Chimeric Molecules Empowers Targeted Protein Ubiquitination and Beyond

Aggie Lawer, Luke Schulz, Renata Sawyer and Xuyu Liu

Cells, 2024, 13, 426
DOI: 10.3390/cells13050426

A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs

Irene Preet Bhela, Alice Ranza, Federica Carolina Balestrero, Marta Serafini, Silvio Aprile, Rita Maria Concetta Di Martino, Fabrizio Condorelli and Tracey Pirali

J. Med. Chem., 2022, 65, 15282
DOI: 10.1021/acs.jmedchem.2c01218

Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB

Elizabeth A. King, Yoojin Cho, Nathan S. Hsu, Dustin Dovala, Jeffrey M. McKenna, John A. Tallarico, Markus Schirle and Daniel K. Nomura

Cell Chemical Biology, 2023, 30, 394
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An overview of PROTACs: a promising drug discovery paradigm

Zi Liu, Mingxing Hu, Yu Yang, Chenghao Du, Haoxuan Zhou, Chengyali Liu, Yuanwei Chen, Lei Fan, Hongqun Ma, Youling Gong and Yongmei Xie

Mol Biomed, 2022, 3
DOI: 10.1186/s43556-022-00112-0

Targeting Apoptosis in AML: Where Do We Stand?

Kinga Krawiec, Piotr Strzałka, Magdalena Czemerska, Aneta Wiśnik, Izabela Zawlik, Agnieszka Wierzbowska and Agnieszka Pluta

Cancers, 2022, 14, 4995
DOI: 10.3390/cancers14204995

PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications

Narayanaperumal Pravin and Krzysztof Jóźwiak

European Journal of Medicinal Chemistry, 2024, 279, 116837
DOI: 10.1016/j.ejmech.2024.116837

Target protein localization and its impact on PROTAC-mediated degradation

Luke M. Simpson, Lorraine Glennie, Abigail Brewer, Jin-Feng Zhao, Jennifer Crooks, Natalia Shpiro and Gopal P. Sapkota

Cell Chemical Biology, 2022, 29, 1482
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Medicinal chemistry strategies targeting viral proteases: From classical design to next-generation therapeutics

Mansour S. Alturki and Mohamed S. Gomaa

European Journal of Medicinal Chemistry, 2026, 310, 118779
DOI: 10.1016/j.ejmech.2026.118779

Discovery of Dual BCL-xL/BCL-w Degraders by Exploiting the Bis(sulfonyl)benzene Ring of ABT-263 as a Linkage Vector

Saikat K. Poddar, Yang Yang, Pratik Pal, Zeng Jin, Jing Pei, Yufeng Xiao, Wanyi Hu, Peiyi Zhang, Praise Adekunbi, Dinesh Thummuri, Yaxia Yuan, Dongwen Lv, J. Peter R. Pelletier, Weizhou Zhang, Daohong Zhou and Guangrong Zheng

J. Med. Chem., 2025, 68, 18684
DOI: 10.1021/acs.jmedchem.5c01834

PROTAC-Mediated Degradation of TAF1 Induces Apoptosis in AML Cells and Inhibits Tumor Growth In Vivo

Lihong Chen, Zachary P. Shultz, Marianna Sansone, Bin Fang, Xiang Liu, Mingxiang Teng, Ernst Schonbrunn, Justin M. Lopchuk and Jiandong Chen

Molecular Cancer Therapeutics, 2025, 24, 1712
DOI: 10.1158/1535-7163.MCT-24-1091

In Silico Tools to Extract the Drug Design Information Content of Degradation Data: The Case of PROTACs Targeting the Androgen Receptor

Giulia Apprato, Giulia D’Agostini, Paolo Rossetti, Giuseppe Ermondi and Giulia Caron

Molecules, 2023, 28, 1206
DOI: 10.3390/molecules28031206

Small-Molecule PROTACs for Cancer Immunotherapy

Zefan Liu, Yajun Zhang, Yucheng Xiang and Xin Kang

Molecules, 2022, 27, 5439
DOI: 10.3390/molecules27175439

Development of Rapid and Facile Solid‐Phase Synthesis of PROTACs via a Variety of Binding Styles

Hanqiao Xu, Takashi Kurohara, Reina Takano, Hidetomo Yokoo, Norihito Shibata, Nobumichi Ohoka, Takao Inoue, Mikihiko Naito and Yosuke Demizu

ChemistryOpen, 2022, 11
DOI: 10.1002/open.202200131

Synthesis, SAR, and application of JQ1 analogs as PROTACs for cancer therapy

Soumik De, Raghaba Sahu, Shubhendu Palei and Laxmi Narayan Nanda

Bioorganic & Medicinal Chemistry, 2024, 112, 117875
DOI: 10.1016/j.bmc.2024.117875

Manipulating autophagic degradation in human diseases: from mechanisms to interventions

Yiqing Zhang, Xiaoxia Liu, Daniel J Klionsky, Boxun Lu and Qing Zhong

Life Medicine, 2022, 1, 120
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Discovery of a potent PROTAC degrader for RNA demethylase FTO as antileukemic therapy

Lu Liu, Yuanlai Qiu, Yuying Suo, Siyao Tong, Yiqing Wang, Xi Zhang, Liang Chen, Yue Huang, Huchen Zhou, Hu Zhou, Ze Dong and Cai-Guang Yang

Acta Pharmaceutica Sinica B, 2024, 14, 5382
DOI: 10.1016/j.apsb.2024.07.016

Recent Advances on Targeting Proteases for Antiviral Development

Pedro Henrique Oliveira Borges, Sabrina Baptista Ferreira and Floriano Paes Silva

Viruses, 2024, 16, 366
DOI: 10.3390/v16030366

Hijacking ERAD for targeted degradation of transmembrane proteins

Haikun Song, Wei Wang, Tingfang Mei, Huiwen Zheng, Keni Ning, Xiaofan Liu, Siulam Cheung, Zhiyuan Cao, Danqi Sheng, Xiaohan Mai, Haoran Zhu, Guankai Guo, Shuaimeng Liu, Rongkai Wei, Qian Wang, Yu Cao, Yu Ding, Yiyan Fei, Rui Liu, Motoyuki Hattori, Chunquan Sheng and Boxun Lu

Cell, 2026, 189, 1768
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Transcription Factors and Cancer

Jamie V. Shiah, Daniel E. Johnson and Jennifer R. Grandis

Cancer J, 2023, 29, 38
DOI: 10.1097/PPO.0000000000000639

Discovery of LHF418 as a new potent SOS1 PROTAC degrader

Huifan Li, Minxue Chai, Yihan Chen, Fengtao Zhou, Xiaomei Ren, Jian Xu, Jian Wang, Zhen Wang and Weixue Huang

Bioorganic & Medicinal Chemistry, 2024, 103, 117661
DOI: 10.1016/j.bmc.2024.117661

Microglial Membrane Camouflaged Nano‐AUTAC to Promote Autophagy‐Mediated β‐Catenin Degradation for Reducing TMZ Resistance in Glioblastoma

Shuai Wu, Ya Wang, Yunfan Li, Minyao Qiu, Yuan Zhong, Maolan Zhang, Haifeng Yang, Jianshu Li and Wei Wu

Adv Funct Materials, 2025
DOI: 10.1002/adfm.202528010

Targeting Oncoproteins for Degradation by Small Molecule-Based Proteolysis-Targeting Chimeras (PROTACs) in Sex Hormone-Dependent Cancers

Li Liu, Lihong Shi, Zhaodi Wang, Jun Zeng, Yue Wang, Hongtao Xiao and Yongxia Zhu

Front. Endocrinol., 2022, 13
DOI: 10.3389/fendo.2022.839857

Recent advances in small molecules targeting the METTL3

Feifei Wu, Lei Yu and Shilin Xu

Future Medicinal Chemistry, 2025, 17, 1933
DOI: 10.1080/17568919.2025.2546781

Structure-Based Discovery of Selective Histone Deacetylase 8 Degraders with Potent Anticancer Activity

Jinbo Huang, Jun Zhang, Wenchao Xu, Qiong Wu, Rongsheng Zeng, Zhichao Liu, Wenhui Tao, Qian Chen, Yongqing Wang and Wei-Guo Zhu

J. Med. Chem., 2023, 66, 1186
DOI: 10.1021/acs.jmedchem.2c00739

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
DOI: 10.1021/acs.jmedchem.3c02135

Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC

Thomas G. Hayhow, Beth Williamson, Mandy Lawson, Natalie Cureton, Erin L. Braybrooke, Andrew Campbell, Rodrigo J. Carbajo, Azadeh Cheraghchi-Bashi, Elisabetta Chiarparin, Coura R. Diène, Charlene Fallan, David I. Fisher, Frederick W. Goldberg, Lorna Hopcroft, Philip Hopcroft, Anne Jackson, Jason G. Kettle, Teresa Klinowska, Ulrike Künzel, Gillian Lamont, Hilary J. Lewis, Gareth Maglennon, Scott Martin, Pablo Morentin Gutierrez, Christopher J. Morrow, Myria Nikolaou, J. Willem M. Nissink, Patrick O’Shea, Radoslaw Polanski, Markus Schade, James S. Scott, Aaron Smith, Judith Weber, Joanne Wilson, Bin Yang and Claire Crafter

Commun Biol, 2024, 7
DOI: 10.1038/s42003-024-06238-x

Beyond CRBN and VHL: Parkin driven lysine-based ternary complexes for selective β3-Tubulin degradation

Sonia Kumari and M. Elizabeth Sobhia

Computers in Biology and Medicine, 2026, 208, 111660
DOI: 10.1016/j.compbiomed.2026.111660

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
DOI: 10.1021/jacs.4c05393

Rewiring the Fusion Oncoprotein EWSR1::FLI1 in Ewing Sarcoma with Bivalent Small Molecules

Michael J. Bond, Ryan P. Golden, Giulia DiGiovanni, Briana Howard, Roman C. Sarott, Basel A. Karim, Sai Gourisankar, Gabriela Alexe, Kenneth Ross, Hannah M. Jones, Brendan G. Dwyer, Nathanael S. Gray and Kimberly Stegmaier

J. Am. Chem. Soc., 2025, 147, 44739
DOI: 10.1021/jacs.5c05634

PROTAC: targeted drug strategy. Principles and limitations

O. A. Koroleva, Yu. V. Dutikova, A. V. Trubnikov, F. A. Zenov, E. V. Manasova, A. A. Shtil and A. V. Kurkin

Russ Chem Bull, 2022, 71, 2310
DOI: 10.1007/s11172-022-3659-z

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
DOI: 10.1021/acs.jmedchem.5c00395

Unlocking the potential of PROTACs: A comprehensive review of protein degradation strategies in disease therapy

Ritesh P. Bhole, Payal R. Kute, Rupesh V. Chikhale, C.G. Bonde, Amit Pant and Shailendra S. Gurav

Bioorganic Chemistry, 2023, 139, 106720
DOI: 10.1016/j.bioorg.2023.106720

Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines

Junjie Hu, Jincui Yang, Runxuan Zhou, Ke Chen, Hongyun Zhao and Yirong Zhou

Biochemical Pharmacology, 2025, 241, 117159
DOI: 10.1016/j.bcp.2025.117159

Structure-based identification of new orally bioavailable BRD9-PROTACs for treating acute myelocytic leukemia

Jingyu Zhang, Haiting Duan, Renzhao Gui, Mingfei Wu, Liteng Shen, Yuheng Jin, Ao Pang, Xiaoli Yu, Shenxin Zeng, Bo Zhang, Nengming Lin, Wenhai Huang, Yuwei Wang, Xiaojun Yao, Jia Li, Xiaowu Dong, Yubo Zhou and Jinxin Che

European Journal of Medicinal Chemistry, 2023, 262, 115872
DOI: 10.1016/j.ejmech.2023.115872

Dégradation induite des protéines par des molécules PROTAC et stratégies apparentées : développements à visée thérapeutique

Michèle Reboud-Ravaux

Biologie Aujourd’hui, 2021, 215, 25
DOI: 10.1051/jbio/2021007

Late-stage synthesis of heterobifunctional molecules for PROTAC applications via ruthenium-catalysed C‒H amidation

Daniele Antermite, Stig D. Friis, Johan R. Johansson, Okky Dwichandra Putra, Lutz Ackermann and Magnus J. Johansson

Nat Commun, 2023, 14
DOI: 10.1038/s41467-023-43789-9

Distal C(sp3)-H Amidation via Ind*RhIII Catalyzed Nitrene Transfer

Hannah J. Ross, Yihui Yu, Liselle Atkin, Milad Ghorbani, Kelly Mint, Nicole Warne, Kristian Kempe and Daniel L. Priebbenow

J. Am. Chem. Soc., 2025, 147, 24734
DOI: 10.1021/jacs.5c06232

PROTAC antibiotics: the time is now

Jickky Palmae Sarathy, Courtney C. Aldrich, Mei-Lin Go and Thomas Dick

Expert Opinion on Drug Discovery, 2023, 18, 363
DOI: 10.1080/17460441.2023.2178413

Roadmap for Optimizing and Broadening Antibody-Based PROTACs for Degradation of Cell Surface Proteins

Josef A. Gramespacher, Adam D. Cotton, Paul W. W. Burroughs, Ian B. Seiple and James A. Wells

ACS Chem. Biol., 2022, 17, 1259
DOI: 10.1021/acschembio.2c00185

Dual Target E3 Ligase Ligands: A New Way to Overcome Drug Resistance

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HJMCe, 2026, 14, 53
DOI: 10.12677/hjmce.2026.141006

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
DOI: 10.1021/jacsau.3c00195

Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer

Chunlan Pu, Yu Tong, Yuanyuan Liu, Suke Lan, Shirui Wang, Guoyi Yan, Hongjia Zhang, Dan Luo, Xinyu Ma, Su Yu, Qing Huang, Rui Deng and Rui Li

European Journal of Medicinal Chemistry, 2022, 236, 114321
DOI: 10.1016/j.ejmech.2022.114321

A comprehensive primer and review of PROTACs and their In Silico design

Jacopo Zattoni, Paola Vottero, Gea Carena, Chiara Uliveto, Giulia Pozzati, Benedetta Morabito, Ebenezea Gitari, Jack Tuszynski and Maral Aminpour

Computer Methods and Programs in Biomedicine, 2025, 264, 108687
DOI: 10.1016/j.cmpb.2025.108687

Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins

Adam G. Bond, Conner Craigon, Kwok-Ho Chan, Andrea Testa, Athanasios Karapetsas, Rotimi Fasimoye, Thomas Macartney, J. Julian Blow, Dario R. Alessi and Alessio Ciulli

J. Med. Chem., 2021, 64, 15477
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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
DOI: 10.1016/j.bioorg.2024.107868

Protein–ligand data at scale to support machine learning

Aled M. Edwards, Dafydd R. Owen, Leili Zhang, Damian W. Young, Timothy M. Willson, James Wellnitz, Yanli Wang, Jarrod Walsh, Erik Vernet, Alexander Tropsha, Claudia Tredup, Matthew H. Todd, Amelia Tjaden, Sven Thamm, Michael Sundström, Andreas Steffen, Shaun Stauffer, Lucas Rodrigo de Souza, Min Shen, Kristof Schütt, Lovisa Holmberg Schiavone, Matthieu Schapira, Santha Santhakumar, Kumar Saikatendu, Emma Rivers, Dušan Petrović, Hui Peng, John P. O’Donnell, Susanne Müller-Knapp, Anke Mueller-Fahrnow, Maxwell R. Morgan, Florian Montel, Juan Carlos Mobarec, Maurice Michel, Sofia Melliou, Uta Lessel, Andrew R. Leach, Oliver Krämer, Florian Krieger, Stefan Knapp, Anthony Keefe, Aimo Kannt, Scott A. Johnson, Sandra Häberle, Emily Rose Holzinger, Ingo V. Hartung, Rachel J. Harding, Thomas Hanke, Levon Halabelian, Benjamin Haibe-Kains, Judith Günther, Marie-Aude Guié, Claudia Gordijo, Opher Gileadi, Luca Foschini, Amaury Fernández-Montalván, Ola Engkvist, Madison M. Edwards, Katharina Duerr, David Drewry, Dengfeng Dou, Snezana Djordjevic, Alejandra Solache Diaz, Sergio Martinez Cuesta, Rafael Counago, Wendy D. Cornell, Jesse A. Coker, Djork-Arné Clevert, Timothy Cernak, Nicola A. Burgess-Brown, Peter J. Brown, Mario H. Bengtson, Frances M. Bashore, Dalia Barsyte-Lovejoy, Arrash J. Baghaie, Alison D. Axtman, Cheryl Arrowsmith, Albert A. Antolin and Suzanne Ackloo

Nat Rev Chem, 2025, 9, 634
DOI: 10.1038/s41570-025-00737-z

Synthesis and biological evaluation of a tumor-selective degrader of PARP1

Chunlan Pu, Shirui Wang, Dan Luo, Yuanyuan Liu, Xinyu Ma, Hongjia Zhang, Su Yu, Suke Lan, Qing Huang, Rui Deng, Xiang He and Rui Li

Bioorganic & Medicinal Chemistry, 2022, 69, 116908
DOI: 10.1016/j.bmc.2022.116908

Recent Advances of Degradation Technologies Based on PROTAC Mechanism

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

Biomolecules, 2022, 12, 1257
DOI: 10.3390/biom12091257

Targeted Protein Degradation via Lysosomes

Rishi R. Paudel, Dong Lu, Sandipan Roy Chowdhury, Erika Y. Monroy and Jin Wang

Biochemistry, 2023, 62, 564
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Recent advances in anticancer mechanisms of molecular glue degraders: focus on RBM39-dgrading synthetic sulfonamide such as indisulam, E7820, tasisulam, and chloroquinoxaline sulfonamide

Ji Hoon Jang, Joo-Young Kim and Tae-Jin Lee

Genes Genom, 2024, 46, 1345
DOI: 10.1007/s13258-024-01565-z

Degradation of LMO2 in T cell leukaemia results in collateral breakdown of transcription complex partners and causes LMO2-dependent apoptosis

Naphannop Sereesongsaeng, Carole Bataille, Angela Russell, Nicolas Bery, Fernando J Sialana, Jyoti Choudhary, Ami Miller and Terence Rabbitts

eLife, 2025, 14
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Targeted Management: Unlocking the Crucial Role of PROTACs in Cancer Treatment

Priyanka Gupta, Sumit Dutta, Prashant Kumar, Monika Kaushik, Sumel Ashique and Mithun Bhowmick

CDDT, 2025, 22
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Recent advances in PROTAC-based antiviral and antibacterial therapeutics

Can Zhou, Shiwei Yang, Jun Wang, Wei Pan, Hongliang Yao, Gang Li and Minhong Niu

Bioorganic Chemistry, 2025, 160, 108437
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Recent Advances in PROTACs for Drug Targeted Protein Research

Tingting Yao, Heng Xiao, Hong Wang and Xiaowei Xu

IJMS, 2022, 23, 10328
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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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In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)

Shusuke Tomoshige and Minoru Ishikawa

Bioorganic & Medicinal Chemistry, 2021, 41, 116221
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Structural insights into human brachyury DNA recognition and discovery of progressible binders for cancer therapy

Joseph A. Newman, Angeline E. Gavard, Nergis Imprachim, Hazel Aitkenhead, Hadley E. Sheppard, Robert te Poele, Paul A. Clarke, Mohammad Anwar Hossain, Louisa Temme, Hans J. Oh, Carrow I. Wells, Zachary W. Davis-Gilbert, Paul Workman, Opher Gileadi and David H. Drewry

Nat Commun, 2025, 16
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Novel strategies and promising opportunities for targeted protein degradation: An innovative therapeutic approach to overcome cancer resistance

Huanjie Zhu, Jin Wang, Qingqing Zhang, Xiaoyan Pan and Jie Zhang

Pharmacology & Therapeutics, 2023, 244, 108371
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Targeted Protein Degradation: Current and Emerging Approaches for E3 Ligase Deconvolution

Yufeng Xiao, Yaxia Yuan, Yi Liu, Zongtao Lin, Guangrong Zheng, Daohong Zhou and Dongwen Lv

J. Med. Chem., 2024, 67, 11580
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Development of PROTACS degrading KRAS and SOS1

GERHARD HAMILTON, MARIE-THERESE EGGERSTORFER and SANDRA STICKLER

OR, 2024, 32, 1257
DOI: 10.32604/or.2024.051653

Multi-targeted pharmacological properties of cinnamyl piperazine derivatives: a comprehensive review

Yongqi Wang, Mengchen Lei, Zefeng Zhao, Shaoping Wu, Xiaohui Zheng, Haifa Qiao and Xiaohang Yang

Med Chem Res, 2025, 34, 19
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The most common linkers in bioactive molecules and their bioisosteric replacement network

Peter Ertl, Eva Altmann and Sophie Racine

Bioorganic & Medicinal Chemistry, 2023, 81, 117194
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VHL-Modified PROteolysis TArgeting Chimeras (PROTACs) as a Strategy to Evade Metabolic Degradation in In Vitro Applications

Beatrice Castellani, Michela Eleuteri, Stefano Di Bona, Gabriele Cruciani, Jenny Desantis and Laura Goracci

J. Med. Chem., 2023, 66, 13148
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Molecular engineering of lysosome-based degraders unveils a rapidly expanding therapeutic strategy

Adele Rivault, Jade Dussart-Gautheret, Rachid Benhida, Anthony R Martin, Patrick Auberger, Arnaud Jacquel and Guillaume Robert

Autophagy, 2026, 1
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Clues to molecular glues

Thomas M. Geiger, Sabine C. Schäfer, Johannes K. Dreizler, Michael Walz and Felix Hausch

Current Research in Chemical Biology, 2022, 2, 100018
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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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Ligandability of E3 Ligases for Targeted Protein Degradation Applications

Bridget P. Belcher, Carl C. Ward and Daniel K. Nomura

Biochemistry, 2023, 62, 588
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Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation

Ryan P. Wurz, Huan Rui, Ken Dellamaggiore, Sudipa Ghimire-Rijal, Kaylee Choi, Kate Smither, Albert Amegadzie, Ning Chen, Xiaofen Li, Abhisek Banerjee, Qing Chen, Dane Mohl and Amit Vaish

Nat Commun, 2023, 14
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Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity

Victoria G. Klein, Adam G. Bond, Conner Craigon, R. Scott Lokey and Alessio Ciulli

J. Med. Chem., 2021, 64, 18082
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Beyond Proteolysis-Targeting Chimeric Molecules: Designing Heterobifunctional Molecules Based on Functional Effectors

Liwen Hua, Qiuyue Zhang, Xinyue Zhu, Ruoning Wang, Qidong You and Lei Wang

J. Med. Chem., 2022, 65, 8091
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In-cell proximity target validation methods for heterobifunctional molecules with CRBN- or VHL-binder using AirID

Kohdai Yamada, Satoshi Yamanaka, Hiroyuki Yamakoshi, Aki Kohyama, Yoshiharu Iwabuchi, Hidetaka Kosako and Tatsuya Sawasaki

Commun Biol, 2025, 8
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Negr1-Derived Peptides Trigger ALK Degradation and Halt Neuroblastoma Progression In Vitro and In Vivo

Francesca Pischedda, Alessia Ghirelli, Vasvi Tripathi and Giovanni Piccoli

Pharmaceutics, 2023, 15, 2307
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Emerging Concepts of Targeted Protein Degrader Technologies via Lysosomal Pathways

Mohammad Maqusood Alam, Sobia Wasim and Sang-Yoon Lee

IJMS, 2025, 26, 5582
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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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PROTACs in Antivirals: Current Advancements and Future Perspectives

Jiacheng Jin, Mengxiang Quan, Xueyan Cao, Yun Zhang, Xiangwei Xu and Zunyuan Wang

Molecules, 2025, 30, 3402
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Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications

Qiong Li, Li Zhou, Siyuan Qin, Zhao Huang, Bowen Li, Ruolan Liu, Mei Yang, Edouard C. Nice, Huili Zhu and Canhua Huang

European Journal of Medicinal Chemistry, 2023, 257, 115447
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Gremlin: a complex molecule regulating wound healing and fibrosis

Steven O’Reilly

Cell. Mol. Life Sci., 2021, 78, 7917
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Targeting EBV Episome for Anti-Cancer Therapy: Emerging Strategies and Challenges

Febri Gunawan Sugiokto and Renfeng Li

Viruses, 2025, 17, 110
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Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders

Jibu Lu, Yongjun Huang, Jing Huang, Rui He, Minhao Huang, Xiaoyun Lu, Yong Xu, Fengtao Zhou, Zhang Zhang and Ke Ding

J. Med. Chem., 2022, 65, 2313
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Tetrazine–trans-cyclooctene ligation: Unveiling the chemistry and applications within the human body

Elisabetta Grazia Tomarchio, Rita Turnaturi, Erika Saccullo, Vincenzo Patamia, Giuseppe Floresta, Chiara Zagni and Antonio Rescifina

Bioorganic Chemistry, 2024, 150, 107573
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PROTAC delivery in tumor immunotherapy: Where are we and where are we going?

Yiyang Li, Yike Wu, Sihan Gao, Tao Sun and Chen Jiang

Journal of Controlled Release, 2025, 378, 116
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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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COVID-19 Therapies: Protease Inhibitions and Novel Degrader Strategies

Michèle Reboud-Ravaux and Chahrazade El Amri

Front. Drug Discov., 2022, 2
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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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From part to whole: AI-driven progress in fragment-based drug discovery

Jinhyeok Yoo, Wonkyeong Jang and Woong-Hee Shin

Current Opinion in Structural Biology, 2025, 91, 102995
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Beyond targeted protein degradation: LD·ATTECs clear cellular lipid droplets

Elena De Vita, Daniel Lucy and Edward W. Tate

Cell Res, 2021, 31, 945
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Targeted protein degradation: A promise for undruggable proteins

Kusal T.G. Samarasinghe and Craig M. Crews

Cell Chemical Biology, 2021, 28, 934
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Protein Degradation Technology

杰克高

HJMCe, 2022, 10, 21
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Targeted Degradation of mRNA Decapping Enzyme DcpS by a VHL-Recruiting PROTAC

Jake C. Swartzel, Michael J. Bond, Andreas P. Pintado-Urbanc, Mehana Daftary, Mackenzie W. Krone, Todd Douglas, Evan J. Carder, Joshua T. Zimmer, Takahiro Maeda, Matthew D. Simon and Craig M. Crews

ACS Chem. Biol., 2022, 17, 1789
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Discovery of novel exceptionally potent and orally active c-MET PROTACs for the treatment of tumors with MET alterations

Pengyun Li, Changkai Jia, Zhiya Fan, Xiaotong Hu, Wenjuan Zhang, Ke Liu, Shiyang Sun, Haoxin Guo, Ning Yang, Maoxiang Zhu, Xiaomei Zhuang, Junhai Xiao, Zhibing Zheng and Song Li

Acta Pharmaceutica Sinica B, 2023, 13, 2715
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Novel Highly Potent c-Met Degraders against a Broad Range of Cancers

Changkai Jia, Pengli Wei, Shiyang Sun, Yaqiu Mao, Ting Wei, Zhenze Qi, Fan Feng, Yalei Wang, Xu Cai, Zhiyuan Zhao, Bingkun Li, Min Qiao, Yaxin Zou, Ziyun Zhang, Tingting Yang, Xiaomei Zhuang, Junhai Xiao, Xuesong Feng, Pengyun Li, Zhibing Zheng and Song Li

J. Med. Chem., 2025, 68, 15176
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Development of visible-light-activatable photocaged PROTACs

Weizhi Weng, Gang Xue and Zhengying Pan

European Journal of Medicinal Chemistry, 2024, 265, 116062
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Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1

Qilong Zhou, Wei Wu, Kaimin Jia, Guangyan Qi, Xiuzhi Susan Sun and Ping Li

European Journal of Medicinal Chemistry, 2022, 244, 114830
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Linker Methylation as a Strategy to Enhance PROTAC Oral Bioavailability: Insights from Molecular Properties and Conformational Analysis

Diego Garcia Jimenez, Giuseppe Ermondi, Zuzana Jandova, Maura Vallaro, Giulia Caron and Heribert Arnhof

J. Med. Chem., 2025, 68, 16666
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Advances and challenges of targeted protein degradation in ophthalmology: Future directions and therapeutic potential

Ke Feng, Mingyan Wei, Panqin Ma, Jiaoyue Hu, Caihong Huang, Yi Han and Zuguo Liu

Materials & Design, 2025, 259, 114767
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The next generation of EGFR inhibitors: a patenting perspective of PROTACs based EGFR degraders

Pengyun Li, Bingkun Li, Ning Yang, Tingting Xu and Zhibing Zheng

Expert Opinion on Therapeutic Patents, 2023, 33, 477
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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, 2026, 30, 353
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Targeted Protein Degradation: Clinical Advances in the Field of Oncology

Abdelrahman K. A. A. Salama, Marija V. Trkulja, Emilio Casanova and Iris Z. Uras

IJMS, 2022, 23, 15440
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Protein Phosphatase 5-Recruiting Chimeras for Accelerating Apoptosis-Signal-Regulated Kinase 1 Dephosphorylation with Antiproliferative Activity

Qiuyue Zhang, Xuexuan Wu, Hengheng Zhang, Qiuyu Wu, Min Fu, Liwen Hua, Xinyue Zhu, Yuqi Guo, Lianshan Zhang, Qidong You and Lei Wang

J. Am. Chem. Soc., 2023, 145, 1118
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Identification of suitable target/E3 ligase pairs for PROTAC development using a rapamycin-induced proximity assay (RiPA)

Bikash Adhikari, Katharina Schneider, Mathias Diebold, Christoph Sotriffer and Elmar Wolf

eLife, 2024, 13
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Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

Siyu Chen, Jingliang Cui, Haiyan Chen, Bo Yu and Sihui Long

European Journal of Medicinal Chemistry, 2023, 262, 115911
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Selection for constrained peptides that bind to a single target protein

Andrew M. King, Daniel A. Anderson, Emerson Glassey, Thomas H. Segall-Shapiro, Zhengan Zhang, David L. Niquille, Amanda C. Embree, Katelin Pratt, Thomas L. Williams, D. Benjamin Gordon and Christopher A. Voigt

Nat Commun, 2021, 12
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PROTACs: Emerging Targeted Protein Degradation Approaches for Advanced Druggable Strategies

Nuwayo Ishimwe Sincere, Krishnan Anand, Sumel Ashique, Jing Yang and Chongge You

Molecules, 2023, 28, 4014
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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
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Targeted Protein Degradation through Recruitment of the CUL4 Complex Adaptor Protein DDB1

Margot Meyers, Sabine Cismoski, Anoohya Panidapu, Barbara Chie-Leon and Daniel K. Nomura

ACS Chem. Biol., 2024, 19, 58
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Towards design of drugs and delivery systems with the Martini coarse-grained model

Lisbeth R. Kjølbye, Gilberto P. Pereira, Alessio Bartocci, Martina Pannuzzo, Simone Albani, Alessandro Marchetto, Brian Jiménez-García, Juliette Martin, Giulia Rossetti, Marco Cecchini, Sangwook Wu, Luca Monticelli and Paulo C. T. Souza

QRB Discovery, 2022, 3
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Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain

Iván Cheng-Sánchez, Katherine A. Gosselé, Leonardo Palaferri, Mariia S. Kirillova and Cristina Nevado

ACS Med. Chem. Lett., 2024, 15, 355
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Systematic Optimization of Proteolysis-Targeting Chimeras for PIN1 Enables Selective Degradation and Antitumor Activity In Vivo

Yuying Ma, Yang Teng, Jinjin Liu, Yuke Deng, Lingbo Xu, Ruichen Gao, Tingyu Peng, Wei Li, Yue Wei, Linfeng Li and Zufeng Guo

Pharmaceutics, 2026, 18, 288
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Design and Synthesis of Pyrrolo[3,4-d]pyrimidine-Based ATR Degraders for Effective Treatment of Colorectal Cancer in Mouse Model

Nian-Dong Mao, Zi Hui, Chen-Chen Wang, Meng-Lan He, Shun-Ran Li, Meng-Qian Yu, Lulu Ye, Jia-Wei Zhou, Zong-Hao Wang, Bo-Qun Du, Guo-Wei Ye, Yu-Qing Zhang, Xia Yao, Xing-Lin Feng, Frédéric Lirussi, Carmen Garrido, Yuan Gao, Hui Luo and Xiang-Yang Ye

J. Med. Chem., 2026, 69, 6902
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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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Replacing a Cereblon Ligand by a DDB1 and CUL4 Associated Factor 11 (DCAF11) Recruiter Converts a Selective Histone Deacetylase 6 PROTAC into a Pan‐Degrader

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

ChemMedChem, 2025, 20
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Ispinesib as an Effective Warhead for the Design of Autophagosome-Tethering Chimeras: Discovery of Potent Degraders of Nicotinamide Phosphoribosyltransferase (NAMPT)

Guoqiang Dong, Ying Wu, Junfei Cheng, Long Chen, Rui Liu, Yu Ding, Shanchao Wu, Junhui Ma and Chunquan Sheng

J. Med. Chem., 2022, 65, 7619
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Major Advances in Emerging Degrader Technologies

Hang Luo, Li Wu, Yujian He, Chong Qin and Xinjing Tang

Front. Cell Dev. Biol., 2022, 10
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Indomethacin-based PROTACs as pan-coronavirus antiviral agents

Jenny Desantis, Beatrice Mercorelli, Marta Celegato, Federico Croci, Alessandro Bazzacco, Massimo Baroni, Lydia Siragusa, Gabriele Cruciani, Arianna Loregian and Laura Goracci

European Journal of Medicinal Chemistry, 2021, 226, 113814
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Targeting the cGAS-STING pathway for therapeutic gain in autoimmune inflammatory cutaneous diseases with a focus on systemic lupus erythematosus and systemic sclerosis

Steven O’Reilly

British Journal of Dermatology, 2025
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First Generation Proteolysis Targeting Chimeras (PROTACs) for the Treatment of Progeria

Jon Macicior‐Michelena, Marcelino Telechea, Daniel Fernández, Alba García‐Martín, Ángeles Canales and Silvia Ortega‐Gutiérrez

Advanced Science, 2026
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Synthesis and degradation effect of PROTACs targeting EGFR triple mutants

Xiao-Xiao Xi, Hong-Yi Zhao, Minhang Xin, Shuai Mao and San-Qi Zhang

Bioorganic & Medicinal Chemistry, 2026, 132, 118427
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PROTACs in Targeted Protein Degradation: Advances in Development and AI-Enhanced Drug Discovery

Mao Du, Tao Liu, Wenyu Wang, Shuai Fan, Mei Tian, Qing Du, Zhidong Wang, Xiaobo Li, Xiaoyu Liu, Qin Xia, Feng Wang and Lei Dong

European Journal of Medicinal Chemistry Reports, 2026, 100332
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Privileged Scaffolds for Potent and Specific Inhibitors of Mono-ADP-Ribosylating PARPs

Maria Giulia Nizi, Chiara Sarnari and Oriana Tabarrini

Molecules, 2023, 28, 5849
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From bench to bedside: current development and emerging trend of KRAS-targeted therapy

Yi Chen, Qiu-pei Liu, Hua Xie and Jian Ding

Acta Pharmacol Sin, 2024, 45, 686
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PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

Xin Han, Wenyi Wei and Yi Sun

Acta Materia Medica, 2022, 1
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Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities

Pritam Maity, Joydeep Chatterjee, Kiran T. Patil, Sahil Arora, Madhurendra K. Katiyar, Manvendra Kumar, Amirreza Samarbakhsh, Gaurav Joshi, Priyadeep Bhutani, Manoj Chugh, Navnath S. Gavande and Raj Kumar

J. Med. Chem., 2023, 66, 3135
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Near‐Infrared Light‐Activated Transcription Factor‐Targeted Proteolysis‐Targeting Chimeras Nanomachine for Targeted Degradation of Transcription Factors

Bei Zhou, Junqing Yang, Bin Zhang, Weishan Wang, Jinbo Li and Yan Zhang

ChemBioChem, 2025, 26
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Strategies for designing proteolysis targeting chimaeras (PROTACs)

Shipeng He, Guoqiang Dong, Junfei Cheng, Ying Wu and Chunquan Sheng

Medicinal Research Reviews, 2022, 42, 1280
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Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor

Rong Hu, Wan-Li Wang, Ying-Yue Yang, Xia-Tong Hu, Qi-Wei Wang, Wei-Qiong Zuo, Ying Xu, Qiang Feng and Ning-Yu Wang

European Journal of Medicinal Chemistry, 2022, 227, 113922
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Dual functionality of MDM2 in PROTACs expands the horizons of targeted protein degradation

Junyi Zhao, Hongzhen Chen and Chao Liang

Biomark Res, 2025, 13
DOI: 10.1186/s40364-025-00826-7

PROTAC-mediated degradation of peroxisomal d-aspartate oxidase: A novel strategy to modulate d-aspartate homeostasis for schizophrenia treatment

Michela Galli, Valentina Rabattoni, Miriam Cavinato, Francesca Vasile, Irene Gado, Kainat Ulfat, Haidi Shehi, Alessandra Silvani, Daniele Passarella, Andrea Citarella, Loredano Pollegioni and Marco Nardini

European Journal of Medicinal Chemistry, 2026, 309, 118720
DOI: 10.1016/j.ejmech.2026.118720

Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope

Sinan Ma, Jianai Ji, Yuanyuan Tong, Yuxuan Zhu, Junwei Dou, Xian Zhang, Shicheng Xu, Tianbao Zhu, Xiaoli Xu, Qidong You and Zhengyu Jiang

Acta Pharmaceutica Sinica B, 2022, 12, 2990
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Digesting the Role of JAK-STAT and Cytokine Signaling in Oral and Gastric Cancers

Yanhong Ni, Jun T. Low, John Silke and Lorraine A. O’Reilly

Front. Immunol., 2022, 13
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Recent Advances in Pro-PROTAC Development to Address On-Target Off-Tumor Toxicity

Chuanjie Chen, Yiwen Yang, Zhe Wang, Huiwen Li, Chanjuan Dong and Xuan Zhang

J. Med. Chem., 2023, 66, 8428
DOI: 10.1021/acs.jmedchem.3c00302

Next‐Generation Proteolysis‐Targeting Chimeras in Precision Oncology: Multifunctional Designs, Emerging Modalities, and Translational Prospects in Targeted Protein Degradation

Mohamed S. Nafie, Mohamed K. Diab, Asmaa S. A. Yassen, Amany M. Elshamy, Mohamed R. El Tohamy, Haytham O. Tawfik and Sherif Ashraf Fahmy

Drug Development Research, 2025, 86
DOI: 10.1002/ddr.70192

Rational Chemical Design of Molecular Glue Degraders

Ethan S. Toriki, James W. Papatzimas, Kaila Nishikawa, Dustin Dovala, Andreas O. Frank, Matthew J. Hesse, Daniela Dankova, Jae-Geun Song, Megan Bruce-Smythe, Heidi Struble, Francisco J. Garcia, Scott M. Brittain, Andrew C. Kile, Lynn M. McGregor, Jeffrey M. McKenna, John A. Tallarico, Markus Schirle and Daniel K. Nomura

ACS Cent. Sci., 2023, 9, 915
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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
DOI: 10.1016/j.drudis.2023.103716

Characterization of preclinical radio ADME properties of ARV-471 for predicting human PK using PBPK modeling

Yifei He, Chenggu Zhu, Peng Lei, Chen Yang, Yifan Zhang, Yuandong Zheng and Xingxing Diao

Journal of Pharmaceutical Analysis, 2025, 15, 101175
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Therapeutic targeting of post-translational modifications in ovarian cancer: mechanisms and clinical applications

Ling Ke and Ying Zhang

J Ovarian Res, 2025, 18
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Making Protein Degradation Visible: Discovery of Theranostic PROTACs for Detecting and Degrading NAMPT

Junfei Cheng, Shipeng He, Jun Xu, Min Huang, Guoqiang Dong and Chunquan Sheng

J. Med. Chem., 2022, 65, 15725
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Discovery of AXL Degraders with Improved Potencies in Triple-Negative Breast Cancer (TNBC) Cells

Rui He, Zhiqiang Song, Yu Bai, Sheng He, Jing Huang, Yongxing Wang, Fengtao Zhou, Weixue Huang, Jing Guo, Zhen Wang, Zheng-Chao Tu, Xiaomei Ren, Zhang Zhang, Jian Xu and Ke Ding

J. Med. Chem., 2023, 66, 1873
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Microtubule‐targeting agents for cancer treatment: Seven binding sites and three strategies

Xingyu Wang, Benoît Gigant, Xi Zheng and Qiang Chen

MedComm – Oncology, 2023, 2
DOI: 10.1002/mog2.46

Target Protein Localisation and Its Impact on PROTAC-Mediated Degradation

Luke Martin Simpson, Lorraine Glennie, Jennifer Crooks, Natalia Shpiro and Gopal Sapkota

SSRN Journal, 2022
DOI: 10.2139/ssrn.4006704

TAC‐tics for Leveraging Proximity Biology in Drug Discovery

Dhanusha A. Nalawansha, Kyle Mangano, Willem den Besten and Patrick Ryan Potts

ChemBioChem, 2024, 25
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Discovery of a Natural Ent-Kaurene Diterpenoid Oridonin as an E3 Ligase Recruiter for PROTACs

Jie Huang, Xuekun Fu, Fang Qiu, Zhijian Liang, Chunhao Cao, Zhuqian Wang, Hongzhen Chen, Siran Yue, Duoli Xie, Yiying Liang, Aiping Lu and Chao Liang

J. Am. Chem. Soc., 2025, 147, 1920
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Deciphering Acetaminophen-Induced Hepatotoxicity: The Crucial Role of Transcription Factors like Nuclear Factor Erythroid 2–Related Factor 2 as Genetic Determinants of Susceptibility to Drug-Induced Liver Injury

Ankit P. Laddha, Hangyu Wu and José E. Manautou

Drug Metabolism and Disposition, 2024, 52, 740
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Hijacking Methyl Reader Proteins for Nuclear-Specific Protein Degradation

Dhanusha A. Nalawansha, Ke Li, John Hines and Craig M. Crews

J. Am. Chem. Soc., 2022, 144, 5594
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Design and Synthesis of Dual-Target Inhibitors Targeting Androgen Receptors and Glucocorticoid Receptors to Overcome Antiandrogen Resistance in Castration-Resistant Prostate Cancer

Chenfan Li, Xiaoli Han, Qiuxia Yan, Yang Ji, Rongyu Zhang, Dazhong Yuan, Fulian Yang, Jianlong Wang, Meng Wu and Jinming Zhou

J. Med. Chem., 2024, 67, 3419
DOI: 10.1021/acs.jmedchem.3c01668

Commentary: PROTACs make undruggable targets druggable: Challenge and opportunity

Bin Lu and Jianpin Ye

Acta Pharmaceutica Sinica B, 2021, 11, 3335
DOI: 10.1016/j.apsb.2021.07.017