Reactive oxygen species-responsive Pre-PROTAC for tumor-specific protein degradation

Haixia Liu, Chaowei Ren, Renhong Sun, Huihui Wang, Yuexiong Zhan, Xiaobao Yang, Biao Jiang and Hongli Chen

Chem. Commun., 2022, 58, 10072
DOI: 10.1039/D2CC03367D

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

Click chemistry in the development of PROTACs

Ce Yang, Ravi Tripathi and Binghe Wang

RSC Chem. Biol., 2024, 5, 189
DOI: 10.1039/D3CB00199G

Developments of CRBN-based PROTACs as potential therapeutic agents

Chao Wang, Yujing Zhang, Yudong Wu and Dongming Xing

European Journal of Medicinal Chemistry, 2021, 225, 113749
DOI: 10.1016/j.ejmech.2021.113749

Recent Advancements in the Discovery of Cereblon-Based Protease-Targeted Chimeras With Potential for Therapeutic Intervention

Harbinder Singh and Devendra K Agrawal

Future Med. Chem., 2022, 14, 1403
DOI: 10.4155/fmc-2022-0149

Progress of small molecules for targeted protein degradation: PROTACs and other technologies

Hong‐Yi Zhao, Minhang Xin and San‐Qi Zhang

Drug Development Research, 2023, 84, 337
DOI: 10.1002/ddr.22026

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
DOI: 10.1080/17460441.2024.2302151

Accelerating the Discovery of Targeted Protein Degraders: Advances in Synthetic Methodologies and Screening Tactics

Baoli Ding, Xiaotong Chen, Yulu Chen, Ji Cao, Bo Yang, Li Jiang and Cheng‐Liang Zhu

Chemistry A European J, 2026, 32
DOI: 10.1002/chem.202503641

In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)

Shusuke Tomoshige and Minoru Ishikawa

Bioorganic & Medicinal Chemistry, 2021, 41, 116221
DOI: 10.1016/j.bmc.2021.116221

A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions

Le Guo, Yaxian Zhou, Xueqing Nie, Zhongrui Zhang, Zhen Zhang, Chunrong Li, Taobo Wang and Weiping Tang

European Journal of Medicinal Chemistry, 2022, 236, 114317
DOI: 10.1016/j.ejmech.2022.114317

A Modular Chemistry Platform for the Development of a Cereblon E3 Ligase‐Based Partial PROTAC Library

Chelsi M. Almodóvar‐Rivera, Zhen Zhang, Jingyao Li, Haibo Xie, Yu Zhao, Le Guo, Marissa G. Mannhardt and Weiping Tang

ChemBioChem, 2023, 24
DOI: 10.1002/cbic.202300482

Bifunctional robots inducing targeted protein degradation

M Elizabeth Sobhia, Harish Kumar and Sonia Kumari

European Journal of Medicinal Chemistry, 2023, 255, 115384
DOI: 10.1016/j.ejmech.2023.115384

Advances of bioorthogonal coupling reactions in drug development

Feiyan Zhan, Jingjie Zhu, Shaowen Xie, Jinyi Xu and Shengtao Xu

European Journal of Medicinal Chemistry, 2023, 253, 115338
DOI: 10.1016/j.ejmech.2023.115338

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

Xuyang Zhao, Yifan Chen, Huang Su and Liqin Zhang

Interdisciplinary Medicine, 2023, 1
DOI: 10.1002/INMD.20230004

Strategies for designing proteolysis targeting chimaeras (PROTACs)

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

Medicinal Research Reviews, 2022, 42, 1280
DOI: 10.1002/med.21877

PROTACs targeting epigenetic proteins

Chao Zhang, Yuna He, Xiuyun Sun, Wenyi Wei, Yanlong Liu and Yu Rao

Acta Materia Medica, 2023, 2
DOI: 10.15212/AMM-2023-0039

Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs

André T. S. Vicente, Sara P. S. P. Moura and Jorge A. R. Salvador

Commun Chem, 2025, 8
DOI: 10.1038/s42004-025-01598-9

Applications and Limitations of Oxime‐Linked “Split PROTACs”

Weijun Gui and Thomas Kodadek

ChemBioChem, 2022, 23
DOI: 10.1002/cbic.202200275

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
DOI: 10.1021/acs.jmedchem.4c02438

Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions

Gang Fan, Shilin Chen, Qingping Zhang, Na Yu, Ziyang Shen, Zhaoji Liu, Weiming Guo, Zhihan Tang, Jing Yang and Miao Liu

MedComm, 2025, 6
DOI: 10.1002/mco2.70401

Proteolysis Targeting Chimeras (PROTACs) Based on Imatinib Induced Degradation of BCR‐ABL in K562 Cells

Chuang Li, Peng Zhang, Gaojie Chang, Mingyue Pan, Fengke Lu, Jiahao Huang, Yanzhi Wang, Qingyan Zhao, Bingxia Sun, Yuting Cui and Feng Sang

ChemistrySelect, 2023, 8
DOI: 10.1002/slct.202300095

Computational analysis of modular diazotransfer reactions for the development of predictive reactivity models and diazotransfer reagents

Meng-Meng Zheng, Liu Cai, Tiancheng Ma, Hao-Dong Tan, Xiaoyu Lai, Jiajia Dong and Xiao-Song Xue

Nat. Synth, 2024, 3, 1507
DOI: 10.1038/s44160-024-00633-2

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

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

Ming He, Chaoguo Cao, Zhihao Ni, Yongbo Liu, Peilu Song, Shuang Hao, Yuna He, Xiuyun Sun and Yu Rao

Sig Transduct Target Ther, 2022, 7
DOI: 10.1038/s41392-022-00999-9

Click Chemistry and Targeted Degradation: A Winning Combination for Medicinal Chemists?

Anna Pasieka, Eleonora Diamanti, Elisa Uliassi and Maria Laura Bolognesi

ChemMedChem, 2023, 18
DOI: 10.1002/cmdc.202300422

A practical “preTACs-cytoblot” platform accelerates the streamlined development of PROTAC-based protein degraders

Zijian Rao, Kailin Li, Ju Hong, Danni Chen, Baoli Ding, Li Jiang, Xuxin Qi, Jiawen Hu, Bo Yang, Qiaojun He, Xiaowu Dong, Ji Cao and Cheng-Liang Zhu

European Journal of Medicinal Chemistry, 2023, 251, 115248
DOI: 10.1016/j.ejmech.2023.115248