Signaling mechanism for receptor-activated canonical transient receptor potential 3 (TRPC3) channels

J Biol Chem. 2003 May 2;278(18):16244-52. doi: 10.1074/jbc.M300544200. Epub 2003 Feb 26.

Abstract

Canonical transient receptor potential 3 (TRPC3) is a receptor-activated, calcium permeant, non-selective cation channel. TRPC3 has been shown to interact physically with the N-terminal domain of the inositol 1,4,5-trisphosphate receptor, consistent with a "conformational coupling" mechanism for its activation. Here we show that low concentrations of agonists that fail to produce levels of inositol 1,4,5-trisphosphate sufficient to induce Ca(2+) release from intracellular stores substantially activate TRPC3. By several experimental approaches, we demonstrate that neither inositol 1,4,5-trisphosphate nor G proteins are required for TRPC3 activation. However, diacylglycerols were sufficient to activate TRPC3 in a protein kinase C-independent manner. Surface receptor agonists and exogenously applied diacylglycerols were not additive in activating TRPC3. In addition, inhibition of metabolism of diacylglycerol slowed the reversal of receptor-dependent TRPC3 activation. We conclude that receptor-mediated activation of phospholipase C in intact cells activates TRPC3 via diacylglycerol production, independently of G proteins, protein kinase C, or inositol 1,4,5-trisphosphate.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Calcium / metabolism
  • Calcium Channels / drug effects
  • Calcium Channels / physiology*
  • Cells, Cultured
  • Diglycerides / metabolism
  • Diglycerides / pharmacology
  • Epidermal Growth Factor / pharmacology
  • GTP-Binding Protein alpha Subunits, Gq-G11
  • Heterotrimeric GTP-Binding Proteins / physiology
  • Humans
  • Inositol 1,4,5-Trisphosphate / pharmacology
  • Inositol 1,4,5-Trisphosphate Receptors
  • Methacholine Chloride / pharmacology
  • Protein Kinase C / physiology
  • Receptors, Cytoplasmic and Nuclear / physiology
  • TRPC Cation Channels
  • Type C Phospholipases / metabolism

Substances

  • Calcium Channels
  • Diglycerides
  • ITPR1 protein, human
  • Inositol 1,4,5-Trisphosphate Receptors
  • Receptors, Cytoplasmic and Nuclear
  • TRPC Cation Channels
  • Methacholine Chloride
  • Epidermal Growth Factor
  • Inositol 1,4,5-Trisphosphate
  • 1-oleoyl-2-acetylglycerol
  • Protein Kinase C
  • Type C Phospholipases
  • GTP-Binding Protein alpha Subunits, Gq-G11
  • Heterotrimeric GTP-Binding Proteins
  • Calcium