辣椒素
TRPV1型
瞬时受体电位通道
生物物理学
化学
对接(动物)
离子通道
结合位点
受体
生物化学
生物
医学
护理部
出处
期刊:Protein & Cell
[Springer Science+Business Media]
日期:2017-01-02
卷期号:8 (3): 169-177
被引量:327
标识
DOI:10.1007/s13238-016-0353-7
摘要
Capsaicin in chili peppers bestows the sensation of spiciness. Since the discovery of its receptor, transient receptor potential vanilloid 1 (TRPV1) ion channel, how capsaicin activates this channel has been under extensive investigation using a variety of experimental techniques including mutagenesis, patch-clamp recording, crystallography, cryo-electron microscopy, computational docking and molecular dynamic simulation. A framework of how capsaicin binds and activates TRPV1 has started to merge: capsaicin binds to a pocket formed by the channel's transmembrane segments, where it takes a "tail-up, head-down" configuration. Binding is mediated by both hydrogen bonds and van der Waals interactions. Upon binding, capsaicin stabilizes the open state of TRPV1 by "pull-and-contact" with the S4-S5 linker. Understanding the ligand-host interaction will greatly facilitate pharmaceutical efforts to develop novel analgesics targeting TRPV1.
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