The Epac1 Protein: Pharmacological Modulators, Cardiac Signalosome and Pathophysiology.

Abstract:

:The second messenger 3',5'-cyclic adenosine monophosphate (cAMP) is one of the most important signalling molecules in the heart as it regulates many physiological and pathophysiological processes. In addition to the classical protein kinase A (PKA) signalling route, the exchange proteins directly activated by cAMP (Epac) mediate the intracellular functions of cAMP and are now emerging as a new key cAMP effector in cardiac pathophysiology. In this review, we provide a perspective on recent advances in the discovery of new chemical entities targeting the Epac1 isoform and illustrate their use to study the Epac1 signalosome and functional characterisation in cardiac cells. We summarize the role of Epac1 in different subcompartments of the cardiomyocyte and discuss how cAMP-Epac1 specific signalling networks may contribute to the development of cardiac diseases. We also highlight ongoing work on the therapeutic potential of Epac1-selective small molecules for the treatment of cardiac disorders.

journal_name

Cells

journal_title

Cells

authors

Bouvet M,Blondeau JP,Lezoualc'h F

doi

10.3390/cells8121543

subject

Has Abstract

pub_date

2019-11-29 00:00:00

issue

12

issn

2073-4409

pii

cells8121543

journal_volume

8

pub_type

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