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Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300.

ABSTRACT: Capturing a coactivator, naturally: the natural products sekikaic acid and lobaric acid, isolated after a high-throughput screen of a structurally diverse extract collection, effectively target the dynamic binding interfaces of the GACKIX domain of the coactivator CBP/p300. These molecules are the most effective inhibitors of the GACKIX domain yet described and are uniquely selective for this domain.

SUBMITTER: Majmudar CY

PROVIDER: S-EPMC3711073 | biostudies-literature | 2012 Nov

REPOSITORIES: biostudies-literature

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Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300.

Majmudar Chinmay Y CY Højfeldt Jonas W JW Arevang Carl J CJ Pomerantz William C WC Gagnon Jessica K JK Schultz Pamela J PJ Cesa Laura C LC Doss Conor H CH Rowe Steven P SP Vásquez Victor V Tamayo-Castillo Giselle G Cierpicki Tomasz T Brooks Charles L CL Sherman David H DH Mapp Anna K AK

Angewandte Chemie (International ed. in English) 20121008 45

Capturing a coactivator, naturally: the natural products sekikaic acid and lobaric acid, isolated after a high-throughput screen of a structurally diverse extract collection, effectively target the dynamic binding interfaces of the GACKIX domain of the coactivator CBP/p300. These molecules are the most effective inhibitors of the GACKIX domain yet described and are uniquely selective for this domain. ...[more]

PMID: 23042634

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