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. 1998 Dec 25;273(52):35238-44.
doi: 10.1074/jbc.273.52.35238.

Degradation of the G protein-coupled receptor kinase 2 by the proteasome pathway

P Penela  1 , A Ruiz-Gómez, J G Castaño, F Mayor Jr
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Free article

Degradation of the G protein-coupled receptor kinase 2 by the proteasome pathway

P Penela et al. J Biol Chem. .
Free article

Abstract

GRK2 is a ubiquitous member of the G protein-coupled receptor kinase (GRK) family and has been shown to play a key role in determining the desensitization and resensitization patterns of a variety of G protein-coupled receptors. In this report, we show that GRK2 is actively degraded by the proteasome proteolytic pathway, unveiling a new mechanism for the rapid regulation of its expression levels. Interestingly, activation of beta2-adrenergic receptors (beta2AR) markedly increases GRK2 ubiquitination and degradation through the proteasome pathway. In addition, blocking GRK2 degradation notably alters beta2AR signaling and internalization, consistent with a relevant physiological role for GRK2 proteasomal degradation. Activity-dependent modulation of GRK2 cellular levels emerges as an important mechanism for modulating the cellular response to agonists acting through G protein-coupled receptors.

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