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Cardiovascular Research 2006 69(1):46-56; doi:10.1016/j.cardiores.2005.09.011
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Copyright © 2005, European Society of Cardiology

Mechanisms of regulation of G protein-coupled receptor kinases (GRKs) and cardiovascular disease

Petronila Penela1, Cristina Murga1, Catalina Ribas1, Antonio S. Tutor, Sandra Peregrín and Federico Mayor, Jr.*

Departamento de Biología Molecular and Centro de Biología Molecular "Severo Ochoa", Consejo Superior de Investigaciones Científicas, Universidad Autónoma de Madrid, 28049 Madrid, Spain

* Corresponding author. Tel.: +34 91 497 4865; fax: +34 91 497 4799. Email address: fmayor{at}cbm.uam.es

The G protein-coupled receptor kinases (GRKs) participate with arrestins in the regulation and signal propagation of multiple G protein-coupled receptors (GPCR) of key physiological and pharmacological relevance in the cardiovascular system. The complex mechanisms of regulation of GRK expression, degradation and function are being unveiled gradually. The levels of these kinases are known to change in pathological situations such as heart failure, hypertrophy and hypertension, and in animal models of these diseases. A better understanding of the mechanisms underlying these changes and of how these alterations participate in the triggering or progression of cardiovascular disease may contribute to the design of novel diagnostic and therapeutic strategies.

KEYWORDS G protein-coupled receptor kinases (GRKs); Heart failure; Protein kinases; Adrenergic receptors; Signal transduction


1 These authors contributed equally to this work.

Time for primary review 31 days


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