EPAC Inhibitors

Exchange proteins directly activated by cAMP (EPAC) are intracellular sensors of cAMP and function as nucleotide exchange factors for the Rap subfamily of Ras GTPases (Rap GEFs). Two EPAC subtypes have been identified: Epac1, encoded by the RAPGEF3 gene, is ubiquitously expressed, while Epac2, encoded by the RAPGEF4, is particularly enriched in the nervous system and in endocrine tissues.

Both Epac1 and Epac2 are composed of two lobes joined by a central region. The N-terminal lobe is ...