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Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors.

ABSTRACT: N,N-Diphenylamines were discovered as potent and selective EPAC2 inhibitors. A study was conducted to determine the structure-activity relationships in a series of inhibitors of which several compounds displayed submicromolar potencies. Selectivity over the related EPAC1 protein was also demonstrated. Computational modeling reveals an allosteric site that is distinct from the cAMP binding domain shared by both EPAC isoforms, providing a theory with regards to subtype selectivity.

SUBMITTER: Wild CT

PROVIDER: S-EPMC4867506 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors.

Wild Christopher T CT Zhu Yingmin Y Na Ye Y Mei Fang F Ynalvez Marcus A MA Chen Haiying H Cheng Xiaodong X Zhou Jia J

ACS medicinal chemistry letters 20160328 5

N,N-Diphenylamines were discovered as potent and selective EPAC2 inhibitors. A study was conducted to determine the structure-activity relationships in a series of inhibitors of which several compounds displayed submicromolar potencies. Selectivity over the related EPAC1 protein was also demonstrated. Computational modeling reveals an allosteric site that is distinct from the cAMP binding domain shared by both EPAC isoforms, providing a theory with regards to subtype selectivity. ...[more]

PMID: 27190593

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