GPCR: G protein complexes--the fundamental signaling assembly

Amino Acids. 2013 Dec;45(6):1303-14. doi: 10.1007/s00726-013-1593-y. Epub 2013 Sep 20.


G protein coupled receptors (GPCR) constitute the largest group of cell surface receptors that transmit various signals across biological membranes through the binding and activation of heterotrimeric G proteins, which amplify the signal and activate downstream effectors leading to the biological responses. Thus, the first critical step in this signaling cascade is the interaction between receptor and its cognate G protein. Understanding this critical event at the molecular level is of high importance because abnormal function of GPCRs is associated with many diseases. Thus, these receptors are targets for drug development.

Publication types

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

MeSH terms

  • Heterotrimeric GTP-Binding Proteins / chemistry*
  • Heterotrimeric GTP-Binding Proteins / metabolism*
  • Humans
  • Models, Molecular
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction*


  • Receptors, G-Protein-Coupled
  • Heterotrimeric GTP-Binding Proteins