Evidence that the TRPV1 S1-S4 membrane domain contributes to thermosensing

Nat Commun. 2020 Aug 20;11(1):4169. doi: 10.1038/s41467-020-18026-2.

Abstract

Sensing and responding to temperature is crucial in biology. The TRPV1 ion channel is a well-studied heat-sensing receptor that is also activated by vanilloid compounds, including capsaicin. Despite significant interest, the molecular underpinnings of thermosensing have remained elusive. The TRPV1 S1-S4 membrane domain couples chemical ligand binding to the pore domain during channel gating. Here we show that the S1-S4 domain also significantly contributes to thermosensing and couples to heat-activated gating. Evaluation of the isolated human TRPV1 S1-S4 domain by solution NMR, far-UV CD, and intrinsic fluorescence shows that this domain undergoes a non-denaturing temperature-dependent transition with a high thermosensitivity. Further NMR characterization of the temperature-dependent conformational changes suggests the contribution of the S1-S4 domain to thermosensing shares features with known coupling mechanisms between this domain with ligand and pH activation. Taken together, this study shows that the TRPV1 S1-S4 domain contributes to TRPV1 temperature-dependent activation.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Binding Sites / genetics
  • Capsaicin / chemistry
  • Capsaicin / metabolism
  • Circular Dichroism
  • Hot Temperature*
  • Humans
  • Ion Channel Gating / genetics
  • Ion Channel Gating / physiology*
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Protein Binding
  • Protein Domains
  • TRPV Cation Channels / chemistry
  • TRPV Cation Channels / genetics
  • TRPV Cation Channels / metabolism*
  • Thermosensing / genetics
  • Thermosensing / physiology*

Substances

  • TRPV Cation Channels
  • TRPV1 protein, human
  • Capsaicin