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QSAR models reveal new EPAC-selective allosteric...
Journal article

QSAR models reveal new EPAC-selective allosteric modulators

Abstract

Exchange proteins directly activated by cAMP (EPAC) are guanine nucleotide exchange factors for the small GTPases, Rap1 and Rap2. They regulate several physiological functions and mitigation of their activity has been suggested as a possible treatment for multiple diseases such as cardiomyopathy, diabetes, chronic pain, and cancer. Several EPAC-specific modulators have been developed, however studies that quantify their structure-activity …

Authors

Mohamed H; Shao H; Akimoto M; Darveau P; MacKinnon MR; Magolan J; Melacini G

Journal

RSC Chemical Biology, Vol. 3, No. 10, pp. 1230–1239

Publisher

Royal Society of Chemistry (RSC)

Publication Date

October 5, 2022

DOI

10.1039/d2cb00106c

ISSN

2633-0679