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Chemistries of bifunctional PROTAC degraders
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2022-08-02 , DOI: 10.1039/d2cs00220e Chaoguo Cao 1, 2 , Ming He 1 , Liguo Wang 1 , Yuna He 1 , Yu Rao 1
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2022-08-02 , DOI: 10.1039/d2cs00220e Chaoguo Cao 1, 2 , Ming He 1 , Liguo Wang 1 , Yuna He 1 , Yu Rao 1
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Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has received extensive attention from both academia and industry as it can potentially access previously inaccessible targets. However, the design and optimization of PROTACs present big challenges for researchers, and the general strategy for its development and optimization is a lot of trial and error based on experience. This review highlights the important advances in this rapidly growing field and critical limitations of the traditional trial-and-error approach to developing PROTACs by analyzing numerous representative examples of PROTACs development. We summarize and analyze the general principles and strategies for PROTACs design and optimization from the perspective of chemical structure design, and propose potential future pathways to facilitate the development of PROTACs.
中文翻译：
双功能 PROTAC 降解剂的化学性质
蛋白水解靶向嵌合体 (PROTACs) 技术是一种新颖且有前途的治疗策略，它使用小分子诱导蛋白质的泛素依赖性降解。它受到了学术界和工业界的广泛关注，因为它有可能访问以前无法访问的目标。然而，PROTACs 的设计和优化对研究人员提出了巨大的挑战，其开发和优化的总体策略是基于经验的大量试错。本综述通过分析 PROTAC 开发的众多代表性实例，强调了这一快速发展领域的重要进展以及传统试错法开发 PROTAC 的关键局限性。
更新日期：2022-08-02
中文翻译：
双功能 PROTAC 降解剂的化学性质
蛋白水解靶向嵌合体 (PROTACs) 技术是一种新颖且有前途的治疗策略，它使用小分子诱导蛋白质的泛素依赖性降解。它受到了学术界和工业界的广泛关注，因为它有可能访问以前无法访问的目标。然而，PROTACs 的设计和优化对研究人员提出了巨大的挑战，其开发和优化的总体策略是基于经验的大量试错。本综述通过分析 PROTAC 开发的众多代表性实例，强调了这一快速发展领域的重要进展以及传统试错法开发 PROTAC 的关键局限性。
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