Selective small-molecule EPAC activators

Urszula Luchowska-Stańska; David Morgan; Stephen J. Yarwood; Graeme Barker

doi:10.1042/BST20190254

Selective small-molecule EPAC activators

Urszula Luchowska-Stańska
, David Morgan
, Stephen J. Yarwood
, Graeme Barker

Research output: Contribution to journal › Article › peer-review

10 Citations (Scopus)

264 Downloads (Pure)

Abstract

The cellular signalling enzymes, EPAC1 and EPAC2, have emerged as key intracellular sensors of the secondary messenger cyclic 3′,5′-adenosine monophosphate (cyclic adenosine monophosphate) alongside protein kinase A. Interest has been galvanised in recent years thanks to the emergence of these species as potential targets for new cardiovascular disease therapies, including vascular inflammation and insulin resistance in vascular endothelial cells. We herein summarise the current state-of-the-art in small-molecule EPAC activity modulators, including cyclic nucleotides, sulphonylureas, and N-acylsulphonamides.

Original language	English
Pages (from-to)	1415-1427
Number of pages	13
Journal	Biochemical Society Transactions
Volume	47
Issue number	5
DOIs	https://doi.org/10.1042/BST20190254
Publication status	Published - 11 Oct 2019

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

cAMP
exchange proteins
signalling

ASJC Scopus subject areas

Biochemistry

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10.1042/BST20190254Licence: CC BY

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© 2019 The Author(s). This is an open access article published by Portland Press Limited on behalf of the Biochemical Society and distributed under the Creative Commons Attribution License 4.0 (CC BY).
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Cite this

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AU - Yarwood, Stephen J.

AU - Barker, Graeme

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AB - The cellular signalling enzymes, EPAC1 and EPAC2, have emerged as key intracellular sensors of the secondary messenger cyclic 3′,5′-adenosine monophosphate (cyclic adenosine monophosphate) alongside protein kinase A. Interest has been galvanised in recent years thanks to the emergence of these species as potential targets for new cardiovascular disease therapies, including vascular inflammation and insulin resistance in vascular endothelial cells. We herein summarise the current state-of-the-art in small-molecule EPAC activity modulators, including cyclic nucleotides, sulphonylureas, and N-acylsulphonamides.

KW - cAMP

KW - exchange proteins

KW - signalling

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JO - Biochemical Society Transactions

JF - Biochemical Society Transactions

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ER -

Selective small-molecule EPAC activators

Abstract

UN SDGs

Keywords

ASJC Scopus subject areas

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