Mechanism of calmodulin inactivation of the calcium-selective TRP channel TRPV6

Sci Adv. 2018 Aug 15;4(8):eaau6088. doi: 10.1126/sciadv.aau6088. eCollection 2018 Aug.

Abstract

Calcium (Ca2+) plays a major role in numerous physiological processes. Ca2+ homeostasis is tightly controlled by ion channels, the aberrant regulation of which results in various diseases including cancers. Calmodulin (CaM)-mediated Ca2+-induced inactivation is an ion channel regulatory mechanism that protects cells against the toxic effects of Ca2+ overload. We used cryo-electron microscopy to capture the epithelial calcium channel TRPV6 (transient receptor potential vanilloid subfamily member 6) inactivated by CaM. The TRPV6-CaM complex exhibits 1:1 stoichiometry; one TRPV6 tetramer binds both CaM lobes, which adopt a distinct head-to-tail arrangement. The CaM carboxyl-terminal lobe plugs the channel through a unique cation-π interaction by inserting the side chain of lysine K115 into a tetra-tryptophan cage at the pore's intracellular entrance. We propose a mechanism of CaM-mediated Ca2+-induced inactivation that can be explored for therapeutic design.

Publication types

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

MeSH terms

  • Animals
  • Binding Sites
  • Calcium / metabolism*
  • Calcium Channels / chemistry*
  • Calcium Channels / metabolism
  • Calmodulin / chemistry*
  • Calmodulin / metabolism
  • Cryoelectron Microscopy
  • Humans
  • Protein Binding
  • Protein Conformation
  • Rats
  • TRPV Cation Channels / antagonists & inhibitors
  • TRPV Cation Channels / chemistry*
  • TRPV Cation Channels / metabolism

Substances

  • Calcium Channels
  • Calmodulin
  • TRPV Cation Channels
  • TRPV6 channel
  • TRPV6 protein, human
  • Calcium