Kinetic scaffolding mediated by a phospholipase C-beta and Gq signaling complex

Science. 2010 Nov 12;330(6006):974-80. doi: 10.1126/science.1193438. Epub 2010 Oct 21.

Abstract

Transmembrane signals initiated by a broad range of extracellular stimuli converge on nodes that regulate phospholipase C (PLC)-dependent inositol lipid hydrolysis for signal propagation. We describe how heterotrimeric guanine nucleotide-binding proteins (G proteins) activate PLC-βs and in turn are deactivated by these downstream effectors. The 2.7-angstrom structure of PLC-β3 bound to activated Gα(q) reveals a conserved module found within PLC-βs and other effectors optimized for rapid engagement of activated G proteins. The active site of PLC-β3 in the complex is occluded by an intramolecular plug that is likely removed upon G protein-dependent anchoring and orientation of the lipase at membrane surfaces. A second domain of PLC-β3 subsequently accelerates guanosine triphosphate hydrolysis by Gα(q), causing the complex to dissociate and terminate signal propagation. Mutations within this domain dramatically delay signal termination in vitro and in vivo. Consequently, this work suggests a dynamic catch-and-release mechanism used to sharpen spatiotemporal signals mediated by diverse sensory inputs.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Catalytic Domain
  • Crystallography, X-Ray
  • Enzyme Activation
  • GTP-Binding Protein alpha Subunits, Gq-G11 / chemistry*
  • GTP-Binding Protein alpha Subunits, Gq-G11 / metabolism*
  • Guanosine Triphosphate / metabolism
  • Humans
  • Hydrogen Bonding
  • Hydrolysis
  • Isoenzymes / chemistry
  • Isoenzymes / metabolism
  • Kinetics
  • Mice
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis
  • Phospholipase C beta / chemistry*
  • Phospholipase C beta / metabolism
  • Protein Binding
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Signal Transduction

Substances

  • Isoenzymes
  • Recombinant Fusion Proteins
  • Guanosine Triphosphate
  • PLCB3 protein, human
  • Phospholipase C beta
  • GTP-Binding Protein alpha Subunits, Gq-G11

Associated data

  • PDB/3OHM