TRPV1通道的药物靶点及多肽类毒素调制剂

Peptide Toxins Targeting to TRPV1 Channel

辣椒素受体TRPV1为瞬时感受器电位通道家族中的成员。作为一种多觉感受器,响应和整合生物体视觉、听觉、温觉、痛觉和触觉等多种感觉相关的渗透压、p H值、机械、离子强度的刺激变化。已发现TRPV1具多个电压和药理活性位点,受H+、ATP、钙调蛋白和多肽等内、外源分子的门控调控。本文聚焦TRPV1及多肽毒素类调制剂的药物靶点选择性,意图推进该通道结构与功能的解析,为靶向TRP通道药物的设计与发现提供科学依据。

TRPV1 is an indispensable member of the transient receptor potential channel family. As being a kind of multiple- sensory receptor,TRPV1 responds to and integrates osmotic,p H,mechanical,temperature,ionic stimuli during visual,auditory,pain,touch and thermal senses. It was found that TRPV1 channels had multiple pharmacological active sites binding H ＋,ATP,calmodulin and peptide molecules. This paper focuses on animal peptide toxins modulating TRPV1 to elucidate their selectivity and interactive mechanisms,which would be helpful to promote our understanding of channel structure and function,design and discovery new drugs targeting to TRP channels.