A powerful bioorthogonal toolbox boosting the development of immune theranostics

Songhan Liu, Chenyu Hua, Xianan Li, Pengcheng Yuan and Bengang Xing

Chem. Sci., 2025, 16, 22870
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Triplet nitrene-mediated photocatalytic azidation of tertiary C(sp3)–H bonds

Noriaki Shimamoto, Norihito Arichi and Hiroaki Ohno

Chem. Commun., 2026, 62, 164
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Proteolysis-targeting drug delivery system (ProDDS): integrating targeted protein degradation concepts into formulation design

Yu Chen, Fengyuan Liu, Samira Pal and Quanyin Hu

Chem. Soc. Rev., 2024, 53, 9582
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Application of a bivalent “click” approach to target tyrosyl-DNA phosphodiesterase 1 (TDP1)

Xue Zhi Zhao, Wenjie Wang, Md Rasel Al Mahmud, Keli Agama, Yves Pommier and Terrence R. Burke

RSC Med. Chem., 2025, 16, 1969
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Signature of click chemistry in advanced techniques for cancer therapeutics

Sherif Shaban Ragab

RSC Adv., 2025, 15, 10583
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Biocompatible Chemistry: A Plug‐and‐Play Toolbox for Chemical Biology Research

Adam R. Lovato, Zeng Lin and Qingfei Zheng

ChemBioChem, 2025, 26
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Fulfilling multiple roles in PROTAC design: The emerging potential of oligonucleotides

Daniel Alencar Rodrigues, Gustavo Salgado Pires, Urbi Roy, Eric Conway and Pedro de Sena Murteira Pinheiro

European Journal of Medicinal Chemistry, 2026, 307, 118688
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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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Recent Advances in the Development of Pro-PROTAC for Selective Protein Degradation

Fady Hakem, Ahmad Abdelwaly, Reem Alshaman, Abdullah Alattar, Fawaz E. Alanazi, Sawsan A. Zaitone and Mohamed A. Helal

Pharmaceutics, 2025, 17, 1160
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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
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Unleashing the Power of Covalent Drugs for Protein Degradation

Meng‐Jie Fu, Hang Jin, Shao‐Peng Wang, Liang Shen, Hong‐Min Liu, Ying Liu, Yi‐Chao Zheng and Xing‐Jie Dai

Medicinal Research Reviews, 2025, 45, 1045
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Mechanistic analysis of diverse click reactions along with their applications

Sushmita Bhatia, Avadh Biharee, Souren Mondal, Swanand Kulkarni, Rakesh Kumar and Suresh Thareja

European Journal of Medicinal Chemistry, 2025, 296, 117800
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Rapid synthesis of proteolysis-targeting chimeras by consecutive click assembly

Yuri Taninaga, Gaku Orimoto, Maho Miyamoto, Kaho Yamada, Hidetomo Yokoo, Yosuke Demizu and Suguru Yoshida

Bulletin of the Chemical Society of Japan, 2025, 98
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Overcoming limitations of targeted protein degraders: developments toward reversible, self-assembling degraders

Elena Valdambrini, Thomas Kodadek, Michael Peel and Francis Barany

Future Medicinal Chemistry, 2026, 18, 729
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PROTAC Technology as a New Tool for Modern Pharmacotherapy

Natalia Kubryń, Łukasz Fijałkowski, Jacek Nowaczyk, Amer Jamil and Alicja Nowaczyk

Molecules, 2025, 30, 2123
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On-demand modular assembly for expedited PROTAC development

Ayan Mukherjee, Vilas D. Kadam, Qi Miao, Wanheng Zhang, Kevin R. MacKenzie, Zhi Tan and Mingxing Teng

Expert Opinion on Drug Discovery, 2024, 19, 769
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Bioorthogonal Chemistry: An Emerging Strategy for Targeted Protein Degradation

Pijun Zhou, Junda Li, Jinyi Xu, Yansong Ren and Shengtao Xu

Chemistry A European J, 2026, 32
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Bifunctional proximity-inducing strategies for targeted and programmable post-translational modifications

Sadiya Tanga, Pallabi Das, Tuhin Baran Samoi, Arpita Hota, Arkadeep Karmakar and Basudeb Maji

Advanced Drug Delivery Reviews, 2026, 115874
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Chemistry-Driven Integrated Innovation: Unleashing the Potential of PROTAC Technology

Hui Xu, Kai Tang, Yuning Song, Luis Menéndez-Arias and Peng Zhan

Pharmaceutical Fronts, 2025, 07, e259
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Modular Assembly of Heterotrifunctional Molecules Enabled by Iodosulfonylation of Allenes and Subsequent Amination

Xiaofeng Lin, Chuxiong Peng, Shijie Liu, Jianpin Xiang, Binyan Lin, Qichen Zhan, Peng Cao and Tao Cao

J. Med. Chem., 2024, 67, 21251
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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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Reversible in-situ assembly of PROTACs using iminoboronate conjugation

Ce Yang, Yayun Xie, Xiaoxiao Yang, Jun Yin and Binghe Wang

Med Chem Res, 2024, 33, 1432
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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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Targeted Protein Degradation in Cancer: PROTACs, New Targets, and Clinical Mechanisms

Bushra Faryal, Zain Ul Abideen, Muhammad Irfan, Haseeb Ahmed, Fazliddin Jalilov, Lola Abduraximova and Ghulam Abbas Ashraf

Biomolecules, 2026, 16, 325
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Applying click chemistry principles to the design of tumor-targeted nanosystems

J. J. Diaz-Mochon and R. M. Sanchez-Martin

Nanomedicine, 2025, 20, 2809
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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 one-pot photocatalytic triazole-based linkerology for PROTACs

Jinhua Liu, Yaqi Deng, Jiabin Yin, Jian Ji, Cong Guan, Xuwen Chen, Xiang Wu, Tong Zhu and Shunying Liu

Cell Reports Physical Science, 2024, 5, 102139
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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
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In silico modeling of targeted protein degradation

Wenxing Lv, Xiaojuan Jia, Bowen Tang, Chao Ma, Xiaopeng Fan, Xurui Jin, Zhangming Niu and Xin Han

European Journal of Medicinal Chemistry, 2025, 289, 117432
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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
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Chuhui Huang, Kate S. Harris, Ghizal Siddiqui and Manuela Jörg

ACS Pharmacol. Transl. Sci., 2025, 8, 978
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Protein Ligases: Nature’s Gift for Protein/Peptide Synthesis

Yvonne Ritsema, Huapeng Li and Qingfei Zheng

BioChem, 2025, 5, 11
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Structure-Informed Design of High-Cooperativity PROTAC Targeting SARS-CoV-2 RdRp via Click Chemistry and Enhanced Sampling Simulations

Kiran Shehzadi, Yue Ran, Iqra Kalsoom, Jingyue Dong, Peifeng Gao, Irfan Muhammad, Ming-Jia Yu, Zihui Meng and Jian-Hua Liang

J. Med. Chem., 2025, 68, 23247
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Targeted Protein Degradation Strategies for Lung Cancers: Focusing on Epidermal Growth Factor Receptor

Min Hou, Mingda Li, Jianghong Zhao, Yanfang Gong, Jing Rong, Zheng Feng, Huanhuan Sun and Jincheng Zeng

Chemistry & Biodiversity, 2026, 23
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Design and development of PROTACs: A new paradigm in anticancer drug discovery

Vishal Mathur, Mukund Jha, Iqra Zai, Moksh Mahajan, Shagufi Nazar, Shaheen Ali, Anam Ilyas, Sana Tanweer, Javed Ali and Ozair Alam

Medicine in Drug Discovery, 2025, 27, 100221
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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
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PROTAC-based protein degradation: a window of opportunity for melanoma therapy

Giulia Gentile, Simona D’Aguanno, Marta Di Martile, Adele Petricca, Elisabetta Valentini, Stefano Scalera and Donatella Del Bufalo

J Biomed Sci, 2026, 33
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