Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe
Digital Object Identifier (DOI)
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.
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Citation / Publisher Attribution
ACS Medicinal Chemistry Letters, v. 9, issue 12, p. 1223-1229
Scholar Commons Citation
Paulson, Carolyn N.; Guan, Xianghong; Ayoub, Alex M.; Chan, Alice; Karim, Rezaul M.; Pomerantz, William C. K.; Schonbrunn, Ernst; Georg, Gunda I.; and Hawkinson, Jon E., "Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe" (2018). Molecular Medicine Faculty Publications. 103.