Targeting G protein-coupled receptor kinases (GRKs) in Heart Failure

Brinks, Henriette; Koch, Walter J (2010). Targeting G protein-coupled receptor kinases (GRKs) in Heart Failure. Drug discovery today - disease mechanisms, 7(2), e129-e134. Amsterdam: Elsevier

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In the human body, over 1000 different G protein-coupled receptors (GPCRs) mediate a broad spectrum of extracellular signals at the plasma membrane, transmitting vital physiological features such as pain, sight, smell, inflammation, heart rate and contractility of muscle cells. Signaling through these receptors is primarily controlled and regulated by a group of kinases, the GPCR kinases (GRKs), of which only seven are known and thus, interference with these common downstream GPCR regulators suggests a powerful therapeutic strategy. Molecular modulation of the kinases that are ubiquitously expressed in the heart has proven GRK2, and also GRK5, to be promising targets for prevention and reversal of one of the most severe pathologies in man, chronic heart failure (HF). In this article we will focus on the structural aspects of these GRKs important for their physiological and pathological regulation as well as well known and novel therapeutic approaches that target these GRKs in order to overcome the development of cardiac injury and progression of HF.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Department of Cardiovascular Disorders (DHGE) > Clinic of Cardiovascular Surgery

UniBE Contributor:

Most, Henriette

Subjects:

600 Technology > 610 Medicine & health

ISSN:

1740-6765

Publisher:

Elsevier

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 14:13

Last Modified:

15 Dec 2014 15:35

PubMed ID:

21218155

URI:

https://boris.unibe.ch/id/eprint/2746 (FactScience: 205620)

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