Structural Properties, Pathophysiological Relevance and Synthetic Modulators of TRPC Channels.

IF 11.6 1区 医学 Q1 CHEMISTRY, MEDICINAL
Xue Qiao, Chunlin Ren, Wumei Wang, Xiaofen Wang, Guo-Bo Li, Cheng Chen, Bengui Ye, Xiaodong Zeng, Yuling Xiao, Xuechuan Hong
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引用次数: 0

Abstract

Transient receptor potential canonical (TRPC) channels, a subfamily of calcium-permeable cation channels, regulate diverse physiological processes and are implicated in disorders including neurological conditions, cardiovascular diseases, and chronic kidney disease. Recent advances in cryo-electron microscopy (cryo-EM) have elucidated TRPC structures, while subtype-selective modulators have clarified their pathophysiological roles and therapeutic potential. This review integrates the structural and functional attributes of TRPC channels, emphasizing their contributions to health and disease. We highlight synthetic strategies and structure-activity relationships driving the development of selective pharmacological tools, several of which show preclinical promise. By uniting TRPC biology with medicinal chemistry, this study provides strategic guidance for advancing clinically viable TRPC-targeted therapeutics.

TRPC通道的结构特性、病理生理相关性和合成调节剂。
瞬时受体电位规范(TRPC)通道是钙渗透阳离子通道的一个亚家族,调节多种生理过程,并与神经系统疾病、心血管疾病和慢性肾病等疾病有关。低温电子显微镜(cryo-EM)的最新进展已经阐明了TRPC的结构,而亚型选择性调节剂已经阐明了它们的病理生理作用和治疗潜力。本文综述了TRPC通道的结构和功能属性,强调了它们对健康和疾病的贡献。我们强调合成策略和结构-活性关系驱动选择性药理工具的发展,其中一些显示临床前的前景。通过将TRPC生物学与药物化学结合起来,本研究为推进临床可行的TRPC靶向治疗提供了战略指导。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
29.30
自引率
0.00%
发文量
52
审稿时长
2 months
期刊介绍: Medicinal Research Reviews is dedicated to publishing timely and critical reviews, as well as opinion-based articles, covering a broad spectrum of topics related to medicinal research. These contributions are authored by individuals who have made significant advancements in the field. Encompassing a wide range of subjects, suitable topics include, but are not limited to, the underlying pathophysiology of crucial diseases and disease vectors, therapeutic approaches for diverse medical conditions, properties of molecular targets for therapeutic agents, innovative methodologies facilitating therapy discovery, genomics and proteomics, structure-activity correlations of drug series, development of new imaging and diagnostic tools, drug metabolism, drug delivery, and comprehensive examinations of the chemical, pharmacological, pharmacokinetic, pharmacodynamic, and clinical characteristics of significant drugs.
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