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AuthorHasan, Slika
AuthorMansour, Hadi
AuthorNasser, Suzanne A.
AuthorShaito, Abdullah
AuthorKobeissy, Firas
AuthorOrekhov, Alexander N.
AuthorPintus, Gianfranco
AuthorEid, Ali H.
Available date2023-03-27T10:39:38Z
Publication Date2023-04-15
Publication NameEuropean Journal of Pharmacology
Identifierhttp://dx.doi.org/10.1016/j.ejphar.2023.175645
CitationSlika H, Mansour H, Nasser SA, Shaito A, Kobeissy F, Orekhov AN, Pintus G, Eid AH. Epac as a tractable therapeutic target. Eur J Pharmacol. 2023 Apr 15;945:175645. doi: 10.1016/j.ejphar.2023.175645.
ISSN00142999
URIhttps://www.sciencedirect.com/science/article/pii/S0014299923001565
URIhttp://hdl.handle.net/10576/41354
AbstractIn 1957, cyclic adenosine monophosphate (cAMP) was identified as the first secondary messenger, and the first signaling cascade discovered was the cAMP-protein kinase A (PKA) pathway. Since then, cAMP has received increasing attention given its multitude of actions. Not long ago, a new cAMP effector named exchange protein directly activated by cAMP (Epac) emerged as a critical mediator of cAMP's actions. Epac mediates a plethora of pathophysiologic processes and contributes to the pathogenesis of several diseases such as cancer, cardiovascular disease, diabetes, lung fibrosis, neurological disorders, and others. These findings strongly underscore the potential of Epac as a tractable therapeutic target. In this context, Epac modulators seem to possess unique characteristics and advantages and hold the promise of providing more efficacious treatments for a wide array of diseases. This paper provides an in-depth dissection and analysis of Epac structure, distribution, subcellular compartmentalization, and signaling mechanisms. We elaborate on how these characteristics can be utilized to design specific, efficient, and safe Epac agonists and antagonists that can be incorporated into future pharmacotherapeutics. In addition, we provide a detailed portfolio for specific Epac modulators highlighting their discovery, advantages, potential concerns, and utilization in the context of clinical disease entities.
SponsorOpen Access funding provided by the Qatar National Library
Languageen
PublisherElsevier
SubjectcAMP
Epac
Cancer
Cardiovascular disease
Pharmacotherapeutics
TitleEpac as a tractable therapeutic target
TypeArticle
Volume Number945
dc.accessType Open Access


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