G-protein-coupled receptor oligomerization and its potential for drug discovery

Nat Rev Drug Discov. 2002 Oct;1(10):808-20. doi: 10.1038/nrd913.


G-protein-coupled receptors (GPCRs) represent by far the largest class of targets for modern drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using assays that presume that these receptors are monomeric. The recent realization that these receptors form homo-oligomeric and hetero-oligomeric complexes has added a new dimension to rational drug design. However, this important aspect of GPCR biology remains largely unincorporated into schemes to search for new therapeutics. This review provides a synopsis of the current thinking surrounding GPCR homo-oligomerization and hetero-oligomerization and shows how new models point towards unexplored avenues in the development of new therapies.

Publication types

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

MeSH terms

  • Animals
  • Drug Delivery Systems* / methods
  • GTP-Binding Proteins / chemistry*
  • GTP-Binding Proteins / metabolism*
  • GTP-Binding Proteins / physiology
  • Humans
  • Receptors, Cell Surface / chemistry*
  • Receptors, Cell Surface / classification
  • Receptors, Cell Surface / metabolism*
  • Receptors, Cell Surface / physiology
  • Structure-Activity Relationship
  • Technology, Pharmaceutical / methods*


  • Receptors, Cell Surface
  • GTP-Binding Proteins