TRPV1：理性药物设计的靶点。
TRPV1: A Target for Rational Drug Design.
机构信息
Institute for Computational Molecular Science, Temple University, Philadelphia, PA 19122, USA.
New Jersey Medical School, Rutgers University, Newark, NJ 07103, USA.
出版信息
Pharmaceuticals (Basel). 2016 Aug 23;9(3):52. doi: 10.3390/ph9030052.
Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca(2+) 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.
瞬时受体电位香草素 1 型（TRPV1）是非选择性、Ca(2+)可渗透的阳离子通道，可被有害热和化学配体（如辣椒素和树脂毒素（RTX））激活。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。本综述将讨论 TRPV1 的拮抗剂和激动剂用于缓解疼痛和其他疾病的基本原理，以及利用新获得的高分辨率结构开发针对该离子通道的新型更好药物的策略。
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