ASMR #1: Identification of a pharmacological inhibitor of Epac1 that protects the heart against acute and chronic models of cardiac stress
Identification of a pharmacological inhibitor of Epac1 that protects the heart against acute and chronic models of cardiac stress Marion Laudette, Antonio Coluccia, Yannis Sainte-Marie, Andrea Solari, Loubina Fazal, Pierre Sicard, Romano Silvestri, Jeanne Mialet-Perez, Sandrine Pons, Bijan Ghaleh, Jean-Paul Blondeau, Frank Lezoualc'h PMID: 30873562 DOI: 10.1093/cvr/cvz076 Abstract Aims: Recent studies reported that cAMP-binding protein Epac1-deficient mice were protected against various forms of cardiac stress, suggesting that pharmacological inhibition of Epac1 could be beneficial for the treatment of cardiac diseases. To test this assumption, we characterized an Epac1-selective inhibitory compound and investigated its potential cardioprotective properties. Methods and results: We used the Epac1-BRET (bioluminescence resonance energy transfer) for searching for non-cyclic nucleotide Epac1 modulators. A thieno[2,3-b]pyridine derivative, designated as AM-001 was identified as a non-...
