Phospholipase C-beta1 directly accelerates GTP hydrolysis by Galphaq and acceleration is inhibited by Gbeta gamma subunits

J Biol Chem. 1999 Jul 9;274(28):19639-43. doi: 10.1074/jbc.274.28.19639.

Abstract

Phospholipase C-beta, the principal effector protein regulated by Galphaq, has been shown to increase the agonist-stimulated, steady-state GTPase activity of Gq in proteoliposomes that contain both heterotrimeric Gq and m1 muscarinic receptor. We now use a moderately stable complex of R183C Galphaq bound to GTP to show that PLC-beta1 acts directly as a GTPase-activating protein (GAP) for isolated Galphaq in a membrane-free system. PLC-beta1 accelerated the hydrolysis of GalphaqR183C.GTP up to 20-fold. The Km was 1.5 nM, which is similar both to the EC50 with which R183C and wild type Galphaq activate PLC-beta1 and to the EC50 with which PLC-beta1 acts as a Gq GAP in the vesicle-based assay. The Galphaq GAP activity of RGS4 can also be quantitated by this assay; it accelerated hydrolysis of bound GTP about 100-fold. The Gq GAP activities of both PLC-beta1 and RGS4 are blocked by Gbeta gamma subunits, probably by a competitive mechanism. These data suggest either that the Gbeta gamma subunits are not continuously required for receptor-catalyzed GDP/GTP exchange during steady-state GTP hydrolysis or that GAPs, either PLC-beta or RGS proteins, can substitute for Gbeta gamma in this set of reactions.

Publication types

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

MeSH terms

  • Animals
  • Binding, Competitive
  • Enzyme Inhibitors / pharmacology
  • GTP-Binding Protein alpha Subunits, Gq-G11
  • GTP-Binding Proteins / genetics
  • GTP-Binding Proteins / metabolism*
  • GTPase-Activating Proteins
  • Guanosine Triphosphate / metabolism*
  • Isoenzymes / metabolism*
  • Kinetics
  • Mice
  • Mutation
  • Phospholipase C beta
  • Protein Binding
  • Proteins / metabolism*
  • RGS Proteins*
  • Signal Transduction
  • Type C Phospholipases / metabolism*

Substances

  • Enzyme Inhibitors
  • GTPase-Activating Proteins
  • Isoenzymes
  • Proteins
  • RGS Proteins
  • RGS4 protein
  • Guanosine Triphosphate
  • Type C Phospholipases
  • Phospholipase C beta
  • Plcb1 protein, mouse
  • GTP-Binding Proteins
  • GTP-Binding Protein alpha Subunits, Gq-G11