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

Carolyn N Paulson, Xianghong Guan, Alex M. Ayoub, Alice Chan, Rezaul M. Karim, William C Pomerantz, Ernst Schönbrunn, Gunda Georg, Jon E. Hawkinson

Research output: Contribution to journalArticle

1 Citation (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)1223-1229
Number of pages7
JournalACS Medicinal Chemistry Letters
Volume9
Issue number12
DOIs
StatePublished - Dec 13 2018

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Fluorescence Polarization
Assays
Screening
Fluorescence
Polarization
Drug Discovery
Structure-Activity Relationship
Throughput
Proteins
Lead
Protein Domains

Keywords

  • BET
  • bromodomain and extra-terminal domain
  • fluorescence polarization
  • pan-BET probe

PubMed: MeSH publication types

  • Journal Article

Cite this

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; Schönbrunn, Ernst; Georg, Gunda; Hawkinson, Jon E.

In: ACS Medicinal Chemistry Letters, Vol. 9, No. 12, 13.12.2018, p. 1223-1229.

Research output: Contribution to journalArticle

Paulson, Carolyn N ; Guan, Xianghong ; Ayoub, Alex M. ; Chan, Alice ; Karim, Rezaul M. ; Pomerantz, William C ; Schönbrunn, Ernst ; Georg, Gunda ; Hawkinson, Jon E. / Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe. In: ACS Medicinal Chemistry Letters. 2018 ; Vol. 9, No. 12. pp. 1223-1229.
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