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Article

Structure-Guided Design of Selective Epac1 and Epac2 Agonists

20 Jan 2015

Abstract excerpt

The second messenger cAMP is known to augment glucose-induced insulin secretion. However, its downstream targets in pancreatic β-cells have not been unequivocally determined. Therefore, we designed cAMP analogues by a structure-guided approach that act as Epac2-selective agonists both in vitro and in vivo. These analogues activate Epac2 about two orders of magnitude more potently than cAMP. The high potency...

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PMID: 25603503
DOI: 10.1371/journal.pbio.1002038

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