Epac signaling protein ligands as tools for studying their biological activity and creating new original drugs
Open Access
- 28 April 2020
- journal article
- Published by Publishing House OKI in Pharmacokinetics and Pharmacodynamics
- No. 4,p. 3-17
- https://doi.org/10.37489/2587-7836-2019-4-3-17
Abstract
The review discusses modern views about the structure and functions of Epac proteins (exchange proteins directly activated by cyclic adenosine monophosphate). The involvement of Epac proteins both in the regulation of the physiological functions of the body and in the initiation of various pathological processes allows to consider them as a fundamentally new biological target for creating original, highly effective drugs. Information on existing Epac protein agonists and antagonists was collected, and the influence of Epac ligands structure on the values of their affinity and selectivity was analyzed. Presumptive mechanisms of the interaction of ligands with Epac proteins are presented.Keywords
This publication has 46 references indexed in Scilit:
- Exchange protein directly activated by cAMP encoded by the mammalian rapgef3 gene: Structure, function and therapeuticsGene, 2015
- Role of Epac in brain and heartBiochemical Society Transactions, 2012
- Spatial Regulation of Cyclic AMP-Epac1 Signaling in Cell Adhesion by ERM ProteinsMolecular and Cellular Biology, 2010
- Epac and PKA: a tale of two intracellular cAMP receptorsActa Biochimica et Biophysica Sinica, 2008
- Epac1 and cAMP-dependent Protein Kinase Holoenzyme Have Similar cAMP Affinity, but Their cAMP Domains Have Distinct Structural Features and Cyclic Nucleotide RecognitionOnline Journal of Public Health Informatics, 2006
- Epac Activation Converts cAMP from a Proliferative into a Differentiation Signal in PC12 CellsMolecular Biology of the Cell, 2005
- Microtubule-Associated Protein 1B-Light Chain 1 Enhances Activation of Rap1 by Exchange Protein Activated by Cyclic AMP but Not Intracellular TargetingMolecular Pharmacology, 2005
- Mechanism of Regulation of the Epac Family of cAMP-dependent RapGEFsOnline Journal of Public Health Informatics, 2000
- A Family of cAMP-Binding Proteins That Directly Activate Rap1Science, 1998
- Epac is a Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMPNature, 1998