Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe

Authors

Carolyn N. Paulson, University of Minnesota
Xianghong Guan, University of Minnesota
Alex M. Ayoub, University of Minnesota
Alice Chan, University of South Florida
Rezaul M. Karim, University of South Florida
William C. K. Pomerantz, University of Minnesota
Ernst Schonbrunn, University of South FloridaFollow
Gunda I. Georg, University of Minnesota
Jon E. Hawkinson, University of Minnesota

Document Type

Article

Publication Date

2018

Digital Object Identifier (DOI)

https://doi.org/10.1021/acsmedchemlett.8b00380

Abstract

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.

Was this content written or created while at USF?

Yes

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.
https://digitalcommons.usf.edu/mme_facpub/103