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Updated: May 18, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300
Chinmay Y Majmudar1, Jonas W Højfeldt, Carl J Arevang
1Department 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.
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