TRPV1: A Target for Rational Drug Design.
TRPV1: A Target for Rational Drug Design.
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DOI：
10.3390/ph9030052
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发表时间：
2016-08-23
期刊：
影响因子：
--
通讯作者：
Rohacs T
中科院分区：
文献类型：
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作者：
Carnevale V;Rohacs T
瞬时受体电位香草素1(TRPV1)是一种非选择性的钙离子通透性阳离子通道，可被有毒的高温和化学配体激活，如辣椒素和树脂毒素(RTX)。已经开发出许多激活或抑制TRPV1的化合物，但没有一种在常规临床实践中使用。这篇综述将讨论TRPV1的拮抗剂和激动剂用于止痛和其他条件的基本原理，以及利用最新可用的高分辨率结构开发针对该离子通道的新的、更好的药物的策略。
Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate or inhibit TRPV1, but none of them are in routine clinical practice. This review will discuss the rationale for antagonists and agonists of TRPV1 for pain relief and other conditions, and strategies to develop new, better drugs to target this ion channel, using the newly available high-resolution structures.