Department of Chemistry, University of Michigan, Ann Arbor, USA.
Angew Chem Int Ed Engl. 2012 Nov 5;51(45):11258-62. doi: 10.1002/anie.201206815. Epub 2012 Oct 8.
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.
捕获共激活因子,顺理成章:经过高通量筛选结构多样的提取物库后分离得到的天然产物色酮酸和洛巴酸,可有效靶向共激活因子 CBP/p300 的 GACKIX 结构域的动态结合界面。这些分子是迄今为止描述的最有效的 GACKIX 结构域抑制剂,并且对该结构域具有独特的选择性。