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.