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Angew Chem Int Ed Engl. 2012 Nov 5;51(45):11258-62. doi: 10.1002/anie.201206815. Epub 2012 Oct 8.

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

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1
Department of Chemistry, University of Michigan, Ann Arbor, USA.

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.

PMID:
23042634
PMCID:
PMC3711073
DOI:
10.1002/anie.201206815
[Indexed for MEDLINE]
Free PMC Article
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