GRK2 at the control shaft of cellular metabolism.

Abstract:

:G protein receptor kinase 2 (GRK2) has been for years mainly considered the negative regulator of the cardiac β adrenergic signaling. However GRK2 is a ubiquitous molecule and its kinase activity and scaffold properties brought to several investigations which have evidenced its involvement in pathophysiology of extra-cardiac diseases. Later discoveries, moreover, indicated that this molecule is also able to influence other pathways such as insulin signaling by an inhibitory role similar to what described years before on βAR signaling. The importance of this novel function is in particular related to the possibility that this molecule can regulate the cellular metabolism, modifying the ability of cells to utilize different substrates. This hypothesis has been recently investigated in animal model of Heart Failure, evidencing that upregulation of GRK2 leads to alterations of cardiac glucose metabolism in the early stages of the disease. However GRK2 shows increased level also in the early stages of others chronic disease such as Alzheimer's Disease, indicating that these findings could be possibly applied to others cellular system and supporting the emerging idea of GRK2 as master regulator of cellular metabolism.

journal_name

Curr Pharm Des

authors

Ciccarelli M,Cipolletta E,Iaccarino G

doi

10.2174/138161212799040493

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

121-7

issue

2

eissn

1381-6128

issn

1873-4286

pii

BSP/CPD/E-PUB000845

journal_volume

18

pub_type

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