Structural insights into the gating mechanisms of TRPV channels

Cell Calcium. 2020 May:87:102168. doi: 10.1016/j.ceca.2020.102168. Epub 2020 Jan 24.

Abstract

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.

Keywords: Cryo-EM; Ion channels; TRP channels; TRPV; X-ray crystallography.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Humans
  • Ion Channel Gating*
  • Models, Molecular
  • Structure-Activity Relationship
  • Transient Receptor Potential Channels / chemistry*
  • Transient Receptor Potential Channels / metabolism*

Substances

  • Transient Receptor Potential Channels