Agonist-independent regulation of constitutively active G-protein-coupled receptors

Trends Biochem Sci. 1998 Nov;23(11):418-22. doi: 10.1016/s0968-0004(98)01287-0.


G-protein-coupled receptors constitute one of the largest protein super-families in mammals. Since the cloning of the encoding genes, these important drug targets have been subjected to thorough biochemical and pharmacological studies. It has become clear that G-protein-coupled receptors not only transmit signals after stimulation by agonists but can also spontaneously couple to signal-transduction pathways. Recent findings show that constitutively active G-protein-coupled receptors can also be regulated in an agonist-independent manner, which has important implications for the interpretation of the actions of (inverse) agonists and the results of site-directed-mutagenesis studies.

Publication types

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

MeSH terms

  • Animals
  • GTP-Binding Proteins / physiology*
  • Humans
  • Receptors, Cell Surface / agonists
  • Receptors, Cell Surface / physiology*


  • Receptors, Cell Surface
  • GTP-Binding Proteins