Structural insights into the gating mechanisms of TRPV channels

[Display omitted] •Structural Biology of TRPV channels.•Binding pockets for ligand activators and inhibitors.•Mechanisms of endogenous channel modulation. Transient Receptor Potential channels from the vanilloid subfamily (TRPV) are a group of cation channels modulated by a variety of endogenous sti...

Full description

Saved in:
Bibliographic Details
Published in:Cell calcium (Edinburgh) 2020-05, Vol.87, p.102168-102168, Article 102168
Main Authors: Pumroy, Ruth A., Fluck, Edwin C., Ahmed, Tofayel, Moiseenkova-Bell, Vera Y.
Format: Article
Language:English
Subjects:
Cryo-EM
Ion channels
TRP channels
TRPV
X-ray crystallography
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] •Structural Biology of TRPV channels.•Binding pockets for ligand activators and inhibitors.•Mechanisms of endogenous channel modulation. Transient Receptor Potential channels from the vanilloid subfamily (TRPV) are a group of cation channels modulated by a variety of endogenous stimuli as well as a range of natural and synthetic compounds. Their roles in human health make them of keen interest, particularly from a pharmacological perspective. However, despite this interest, the complexity of these channels has made it difficult to obtain high resolution structures until recently. With the cryo-EM resolution revolution, TRPV channel structural biology has blossomed to produce dozens of structures, covering every TRPV family member and a variety of approaches to examining channel modulation. Here, we review all currently available TRPV structures and the mechanistic insights into gating that they reveal.
ISSN:0143-4160
1532-1991
DOI:10.1016/j.ceca.2020.102168