期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 57, 期 9, 页码 3651-3665出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm401425e
关键词
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资金
- National Institutes of Health [R01 GM106218, R01 GM066170, R21 NS066510, P30 DA028821, R21 MH093844]
- R. A. Welch Foundation Chemistry, and Biology Collaborative Grant from Gulf Coast Consortia (GCC) for Chemical Genomics
- Keck Center for Interdisciplinary Bioscience Training of the GCC (NIGMS) [T32 GM089657]
- John Sealy Memorial Endowment Fund
- Technology Development Foundation of Fuzhou University [2013-XQ-8, 2013-XQ-9]
3',5'-Cyclic adenosine monophosphate (cAMP) is a pivotal second messenger that regulates numerous biological processes under physiological and pathological conditions, including cancer, diabetes, heart failure, inflammation, and neurological disorders. In the past, all effects of cAMP were initially believed to be mediated by protein kinase A (PKA) and cyclic nucleotide-regulated ion channels. Since the discovery of exchange proteins directly activated by cyclic adenosine 5'-monophosphate (EPACs) in 1998, accumulating evidence has demonstrated that the net cellular effects of cAMP are also regulated by EPAC. The pursuit of the biological functions of EPAC has benefited from the development and applications of a growing number of pharmacological probes targeting EPACs. In this review, we seek to provide a concise update on recent advances in the development of chemical entities including various membrane-permeable analogues of cAMP and newly discovered EPAC-specific ligands from high throughput assays and hit-to-lead optimizations.
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