Paulson Carolyn N, Guan Xianghong, Ayoub Alex M, Chan Alice, Karim Rezaul M, Pomerantz William C K, Schönbrunn Ernst, Georg Gunda I, Hawkinson Jon E
Department of Medicinal Chemistry and Institute for Therapeutics Discovery & Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.
Department of Chemistry, University of Minnesota, 207 Pleasant Street, SE, Minneapolis, Minnesota 55455, United States.
ACS Med Chem Lett. 2018 Oct 31;9(12):1223-1229. doi: 10.1021/acsmedchemlett.8b00380. eCollection 2018 Dec 13.
Several chemical probes have been developed for use in fluorescence polarization screening assays to aid in drug discovery for the bromodomain and extra-terminal domain (BET) proteins. However, few of those have been characterized in the literature. We have designed, synthesized, and thoroughly characterized a novel fluorescence polarization pan-BET chemical probe suitable for high-throughput screening, structure-activity relationships, and hit-to-lead potency and selectivity assays to identify and characterize BET bromodomain inhibitors.
已经开发了几种化学探针用于荧光偏振筛选测定，以辅助针对溴结构域和额外末端结构域（BET）蛋白的药物发现。然而，其中很少有在文献中得到表征。我们设计、合成并全面表征了一种新型的荧光偏振泛BET化学探针，适用于高通量筛选、构效关系研究以及从苗头化合物到先导化合物的效力和选择性测定，以鉴定和表征BET溴结构域抑制剂。
