Parnell, E., Palmer, T. M. and Yarwood, S. J. (2015) The future of EPAC-targeted therapeutics: agonism versus antagonism. Trends in Pharmacological Sciences, 36(4), pp. 203-214. (doi: 10.1016/j.tips.2015.02.003) (PMID:25744542) (PMCID:PMC4392396)
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Abstract
Pharmaceutical manipulation of cyclic adenosine monophosphate (cAMP) levels exerts beneficial effects through the regulation of the exchange protein activated by cAMP (EPAC) and protein kinase A (PKA) signalling routes. Recent attention has turned to the specific regulation of EPAC isoforms (EPAC1 and EPAC2) as a more targeted approach to cAMP-based therapeutics. For example, EPAC2-selective agonists could promote insulin secretion from pancreatic beta-cells, whereas EPAC1-selective agonists may be useful in the treatment of vascular inflammation. In contrast, EPAC1 and EPAC2 antagonists could both be useful in the treatment of heart failure. Here we discuss whether the best way forward is to design EPAC-selective agonists or antagonists and the current strategies being used to develop isoform-selective, small molecule regulators of EPAC1 and EPAC2 activity.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Yarwood, Dr Stephen and Palmer, Dr Timothy and Parnell, Mr Euan |
| Authors: | Parnell, E., Palmer, T. M., and Yarwood, S. J. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Cardiovascular & Metabolic Health College of Medical Veterinary and Life Sciences > School of Molecular Biosciences |
| Journal Name: | Trends in Pharmacological Sciences |
| Publisher: | Elsevier Inc. |
| ISSN: | 0165-6147 |
| ISSN (Online): | 1873-3735 |
| Copyright Holders: | Copyright © 2015 The Authors |
| First Published: | First published in Trends in Pharmacological Sciences 36(4):203-214 |
| Publisher Policy: | Reproduced under a Creative Commons License |
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