Recent advances in developing targeted protein degraders,European Journal of Medicinal Chemistry

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Recent advances in developing targeted protein degraders
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-12-27 , DOI: 10.1016/j.ejmech.2024.117212
Binbin Cheng ₁ , Hongqiao Li ₂ , Xiaopeng Peng ₃ , Jianjun Chen ₄ , Chuxiao Shao ₅ , Zhihua Kong ₆

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Targeted protein degradation (TPD) represents a promising therapeutic approach, encompassing several innovative strategies, including but not limited to proteolysis targeting chimeras (PROTACs), molecular glues, hydrophobic tag tethering degraders (HyTTD), and lysosome-targeted chimeras (LYTACs). Central to TPD are small molecule ligands, which play a critical role in mediating the degradation of target proteins. This review summarizes the current landscape of small molecule ligands for TPD molecules. These small molecule ligands can utilize the proteasome, lysosome, autophagy, or hydrophobic-tagging system to achieve the degradation of target proteins. The article mainly focuses on introducing their design principles, application advantages, and potential limitations. A brief discussion on the development prospects and future directions of TPD technology was also provided.

中文翻译：

靶向蛋白降解剂开发的最新进展

靶向蛋白降解（TPD）是一种很有前途的治疗方法，包括多种创新策略，包括但不限于蛋白水解靶向嵌合体（PROTAC）、分子胶、疏水性标签栓系降解剂（HyTTD）和溶酶体靶向嵌合体（LYTAC）。TPD 的核心是小分子配体，它在介导靶蛋白的降解中起着关键作用。本文总结了 TPD 分子小分子配体的现状。这些小分子配体可以利用蛋白酶体、溶酶体、自噬或疏水标记系统来实现靶蛋白的降解。本文主要重点介绍了他们的设计原则、应用优势和潜在的局限性。还简要讨论了 TPD 技术的发展前景和未来方向。

更新日期：2024-12-27

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