Physiological roles of G protein–coupled receptor kinases and arrestins

RT Premont, RR Gainetdinov - Annu. Rev. Physiol., 2007 - annualreviews.org
Heterotrimeric G protein–coupled receptors (GPCRs) are found on the surface of all cells of
multicellular organisms and are major mediators of intercellular communication. More than
800 distinct GPCRs are present in the human genome, and individual receptor subtypes
respond to hormones, neurotransmitters, chemokines, odorants, or tastants. GPCRs
represent the most widely targeted pharmacological protein class. Because drugs that target
GPCRs often engage receptor regulatory mechanisms that limit drug effectiveness …