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

Angew Chem Int Ed Engl 2012 Nov 8;51(45):11258-62. Epub 2012 Oct 8.

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

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.

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http://dx.doi.org/10.1002/anie.201206815DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3711073PMC
November 2012
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