Selective small-molecule EPAC activators
Urszula Luchowska-Stańska1, David Morgan2, Stephen J Yarwood1
1Institute of Biological Chemistry, Biophysics, and Bioengineering, Heriot-Watt University, Edinburgh EH14 4AS, U.K.
Abstract:
The cellular signalling enzymes, EPAC1 and EPAC2, have emerged as key intracellular sensors of the secondary messenger cyclic 3',5'-adenosine monophosphate (cyclic adenosine monophosphate) alongside protein kinase A. Interest has been galvanised in recent years thanks to the emergence of these species as potential targets for new cardiovascular disease therapies, including vascular inflammation and insulin resistance in vascular endothelial cells. We herein summarise the current state-of-the-art in small-molecule EPAC activity modulators, including cyclic nucleotides, sulphonylureas, and N-acylsulphonamides.
Related Concept Videos
GPCRs Regulate Adenylyl Cylase Activity
cAMP-dependent Protein Kinase Pathways
GTPases and their Regulation
Large G-proteins,...
Amplifying Signals via Enzymatic Cascade
Adrenergic Agonists: Direct-Acting Agents
These agents can be classified...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...


