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Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe.
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.
Afiliación
  • Paulson CN; 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.
  • Guan X; 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.
  • Ayoub AM; Department of Chemistry, University of Minnesota, 207 Pleasant Street, SE, Minneapolis, Minnesota 55455, United States.
  • Chan A; H. Lee Moffitt Cancer Center & Research Institute, 12902 Magnolia Drive, Tampa, Florida 33612, United States.
  • Karim RM; Department of Molecular Medicine, University of South Florida, Tampa, Florida 33612, United States.
  • Pomerantz WCK; H. Lee Moffitt Cancer Center & Research Institute, 12902 Magnolia Drive, Tampa, Florida 33612, United States.
  • Schönbrunn E; Department of Molecular Medicine, University of South Florida, Tampa, Florida 33612, United States.
  • Georg GI; Department of Chemistry, University of Minnesota, 207 Pleasant Street, SE, Minneapolis, Minnesota 55455, United States.
  • Hawkinson JE; H. Lee Moffitt Cancer Center & Research Institute, 12902 Magnolia Drive, Tampa, Florida 33612, United States.
ACS Med Chem Lett ; 9(12): 1223-1229, 2018 Dec 13.
Article en En | MEDLINE | ID: mdl-30613330
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.
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Texto completo: 1 Bases de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2018 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2018 Tipo del documento: Article País de afiliación: Estados Unidos