G protein βγ subunits: central mediators of G protein-coupled receptor signaling

Cell Mol Life Sci. 2008 Jul;65(14):2191-214. doi: 10.1007/s00018-008-8006-5.


G protein betagamma subunits are central participants in G protein-coupled receptor signaling pathways. They interact with receptors, G protein alpha subunits and downstream targets to coordinate multiple, different GPCR functions. Much is known about the biology of Gbetagamma subunits but mysteries remain. Here, we will review what is known about general aspects of structure and function of Gbetagamma as well as discuss emerging mechanisms for regulation of Gbetagamma signaling. Recent data suggest that Gbetagamma is a potential therapeutic drug target. Thus, a thorough understanding of the molecular and physiological functions of Gbetagamma has significant implications.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Crystallography, X-Ray
  • Drug Evaluation, Preclinical
  • GTP-Binding Protein alpha Subunits / chemistry
  • GTP-Binding Protein alpha Subunits / metabolism*
  • GTP-Binding Protein gamma Subunits / chemistry
  • GTP-Binding Protein gamma Subunits / metabolism*
  • Humans
  • Models, Biological
  • Models, Molecular
  • Multiprotein Complexes
  • Peptide Mapping
  • Pertussis Toxin / toxicity
  • Protein Interaction Mapping
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction / drug effects
  • Static Electricity


  • GTP-Binding Protein alpha Subunits
  • GTP-Binding Protein gamma Subunits
  • Multiprotein Complexes
  • Receptors, G-Protein-Coupled
  • Pertussis Toxin