Selective small-molecule EPAC activators

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

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)1415-1427
Number of pages13
JournalBiochemical Society Transactions
Volume47
Issue number5
DOIs
Publication statusPublished - 11 Oct 2019

Fingerprint

Cyclic Nucleotides
Adenosine Monophosphate
Cyclic AMP-Dependent Protein Kinases
Vascular Resistance
Insulin Resistance
Cardiovascular Diseases
Endothelial Cells
Inflammation
Enzymes
Therapeutics
erythromycin propionate-N-acetylcysteinate
adenosine monophosphate-adenosine

Keywords

  • cAMP
  • exchange proteins
  • signalling

ASJC Scopus subject areas

  • Biochemistry

Cite this

Luchowska-Stańska, Urszula ; Morgan, David ; Yarwood, Stephen J. ; Barker, Graeme. / Selective small-molecule EPAC activators. In: Biochemical Society Transactions. 2019 ; Vol. 47, No. 5. pp. 1415-1427.
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Selective small-molecule EPAC activators. / Luchowska-Stańska, Urszula; Morgan, David; Yarwood, Stephen J.; Barker, Graeme.

In: Biochemical Society Transactions, Vol. 47, No. 5, 11.10.2019, p. 1415-1427.

Research output: Contribution to journalArticle

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