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BIBTEX RIS

G PROTEIN–COUPLED RECEPTOR KINASES

1998; Annual Reviews; Volume: 67; Issue: 1 Linguagem: Inglês

10.1146/annurev.biochem.67.1.653

ISSN

1545-4509

Autores

Julie A. Pitcher, Neil J. Freedman, Robert J. Lefkowitz,

Tópico(s)

Renin-Angiotensin System Studies

Resumo

G protein-coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein-coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization. This review focuses on the regulation of GRK activity by a variety of allosteric and other factors: agonist-stimulated GPCRs, beta gamma subunits of heterotrimeric GTP-binding proteins, phospholipid cofactors, the calcium-binding proteins calmodulin and recoverin, posttranslational isoprenylation and palmitoylation, autophosphorylation, and protein kinase C-mediated GRK phosphorylation. Studies employing recombinant, purified proteins, cell culture, and transgenic animal models attest to the general importance of GRKs in regulating a vast array of GPCRs both in vitro and in vivo.

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