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Small molecules targeting canonical transient receptor potential channels: an update
Drug Discovery Today ( IF 7.4 ) Pub Date : 2024-03-20 , DOI: 10.1016/j.drudis.2024.103951
Hua Liu , Min Fu , Yifan Zhang , Qidong You , Lei Wang

Transient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different subtypes of TRPC, including potential preclinical drug candidates. This review covers recent advancements in the understanding of TRPC regulation and structure and the discovery of TRPC small molecules over the past few years, with the aim of facilitating research on TRPCs and small-molecule drug discovery.

中文翻译:

靶向经典瞬时受体电位通道的小分子:更新

瞬时受体电位规范(TRPC)通道属于一类重要的非选择性阳离子通道。该通道家族由多个成员组成,广泛参与各种生理和病理过程。先前的研究揭示了这些通道的复杂调控,以及 TRPC 的空间排列和各种小分子化合物的结合位点。多种小分子已被确定为针对 TRPC 不同亚型的选择性激动剂或抑制剂,包括潜在的临床前候选药物。本综述涵盖了过去几年对 TRPC 调控和结构的理解以及 TRPC 小分子的发现的最新进展,旨在促进 TRPC 的研究和小分子药物的发现。
更新日期:2024-03-20
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