Conway Stuart J
EaStCHEM, School of Chemistry, Centre for Biomolecular Sciences, University of St Andrews, North Haugh, St Andrews, UK.
Chem Soc Rev. 2008 Aug;37(8):1530-45. doi: 10.1039/b610226n. Epub 2008 Jun 20.
Capsaicin has elicited great interest for many centuries due to its noticeable culinary and medical properties. The discovery of its receptor, TRPV1, sparked an explosion of interest in TRPV1 and the development of TRPV1 agonists and antagonists. This tutorial review provides an introduction to the history of both capsaicin and TRPV1. Two TRPV1 antagonists that are undergoing clinical trials are highlighted, as are some light-activated molecular tools that are enabling the intracellular study of this protein. This article will be of interest to chemists and biologists with an interest in TRPV1, cell signalling, or medicinal and biological chemistry.
几个世纪以来,辣椒素因其显著的烹饪和医学特性而备受关注。其受体TRPV1的发现引发了对TRPV1以及TRPV1激动剂和拮抗剂开发的极大兴趣。本教程综述介绍了辣椒素和TRPV1的历史。重点介绍了两种正在进行临床试验的TRPV1拮抗剂,以及一些能够对该蛋白进行细胞内研究的光激活分子工具。本文将引起对TRPV1、细胞信号传导、药物化学和化学生物学感兴趣的化学家和生物学家的关注。