Arresting developments in heptahelical receptor signaling and regulation

Trends Cell Biol. 2002 Mar;12(3):130-8. doi: 10.1016/s0962-8924(01)02239-5.


It is well established that the function of most heptahelical receptors (seven-transmembrane-span receptors; 7TMRs) is tightly regulated by the desensitizing actions of arrestins. Desensitization is the waning of 7TMR-mediated signals after prolonged exposure to agonist and occurs when arrestins bind to agonist-occupied and phosphorylated receptors, uncoupling the receptors from G proteins and preventing further signaling. Recently, there has been a marked shift in the focus of research into arrestin function because it has become clear that they not only prevent signaling from 7TMRs but also initiate and direct new signals from the very 7TMRs that they desensitize.

Publication types

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

MeSH terms

  • Animals
  • Arrestins / metabolism
  • Arrestins / pharmacology
  • Arrestins / physiology*
  • GTP-Binding Proteins / metabolism
  • GTP-Binding Proteins / physiology
  • Humans
  • Receptors, Cell Surface / metabolism
  • Receptors, Cell Surface / physiology
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*


  • Arrestins
  • Receptors, Cell Surface
  • GTP-Binding Proteins