Literature DB >> 30613330

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

Carolyn N Paulson1, Xianghong Guan1, Alex M Ayoub2, Alice Chan3,4, Rezaul M Karim3,4, William C K Pomerantz2, Ernst Schönbrunn3,4, Gunda I Georg1, Jon E Hawkinson1.   

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.

Entities:  

Year:  2018        PMID： 30613330      PMCID： PMC6295860          DOI： 10.1021/acsmedchemlett.8b00380

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  28 in total

Review 1.  Bromodomain: an acetyl-lysine binding domain.

Authors:  Lei Zeng; Ming Ming Zhou
Journal:  FEBS Lett       Date:  2002-02-20       Impact factor: 4.124

Review 2.  Fluorescence polarization/anisotropy in diagnostics and imaging.

Authors:  David M Jameson; Justin A Ross
Journal:  Chem Rev       Date:  2010-05-12       Impact factor: 60.622

Review 3.  Chromatin modifications and their function.

Authors:  Tony Kouzarides
Journal:  Cell       Date:  2007-02-23       Impact factor: 41.582

4.  Spectral dispersion and water solubilization of BODIPY dyes via palladium-catalyzed C-H functionalization.

Authors:  Cliferson Thivierge; Rakeshwar Bandichhor; Kevin Burgess
Journal:  Org Lett       Date:  2007-04-25       Impact factor: 6.005

5.  BODIPY derivatives as donor materials for bulk heterojunction solar cells.

Authors:  Theodulf Rousseau; Antonio Cravino; Thomas Bura; Gilles Ulrich; Raymond Ziessel; Jean Roncali
Journal:  Chem Commun (Camb)       Date:  2009-02-11       Impact factor: 6.222

6.  Discovery and characterization of small molecule inhibitors of the BET family bromodomains.

Authors:  Chun-Wa Chung; Herve Coste; Julia H White; Olivier Mirguet; Jonathan Wilde; Romain L Gosmini; Chris Delves; Sylvie M Magny; Robert Woodward; Stephen A Hughes; Eric V Boursier; Helen Flynn; Anne M Bouillot; Paul Bamborough; Jean-Marie G Brusq; Francoise J Gellibert; Emma J Jones; Alizon M Riou; Paul Homes; Sandrine L Martin; Iain J Uings; Jerome Toum; Catherine A Clement; Anne-Benedicte Boullay; Rachel L Grimley; Florence M Blandel; Rab K Prinjha; Kevin Lee; Jorge Kirilovsky; Edwige Nicodeme
Journal:  J Med Chem       Date:  2011-05-13       Impact factor: 7.446

7.  Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization.

Authors:  Zaneta Nikolovska-Coleska; Renxiao Wang; Xueliang Fang; Hongguang Pan; York Tomita; Peng Li; Peter P Roller; Krzysztof Krajewski; Naoyuki G Saito; Jeanne A Stuckey; Shaomeng Wang
Journal:  Anal Biochem       Date:  2004-09-15       Impact factor: 3.365

8.  The first bromodomain of Brdt, a testis-specific member of the BET sub-family of double-bromodomain-containing proteins, is essential for male germ cell differentiation.

Authors:  Enyuan Shang; Helen D Nickerson; Duancheng Wen; Xiangyuan Wang; Debra J Wolgemuth
Journal:  Development       Date:  2007-08-29       Impact factor: 6.868

9.  Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.

Authors:  Martin Philpott; Jing Yang; Tony Tumber; Oleg Fedorov; Sagar Uttarkar; Panagis Filippakopoulos; Sarah Picaud; Tracy Keates; Ildiko Felletar; Alessio Ciulli; Stefan Knapp; Tom D Heightman
Journal:  Mol Biosyst       Date:  2011-08-01

10.  Selective inhibition of BET bromodomains.

Authors:  Panagis Filippakopoulos; Jun Qi; Sarah Picaud; Yao Shen; William B Smith; Oleg Fedorov; Elizabeth M Morse; Tracey Keates; Tyler T Hickman; Ildiko Felletar; Martin Philpott; Shonagh Munro; Michael R McKeown; Yuchuan Wang; Amanda L Christie; Nathan West; Michael J Cameron; Brian Schwartz; Tom D Heightman; Nicholas La Thangue; Christopher A French; Olaf Wiest; Andrew L Kung; Stefan Knapp; James E Bradner
Journal:  Nature       Date:  2010-09-24       Impact factor: 49.962
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  1 in total

1.  Quantifying the Selectivity of Protein-Protein and Small Molecule Interactions with Fluorinated Tandem Bromodomain Reader Proteins.

Authors:  Prakriti Kalra; Logan McGraw; Jennifer R Kimbrough; Anil K Pandey; Jonathan Solberg; Huarui Cui; Anand Divakaran; Kristen John; Jon E Hawkinson; William C K Pomerantz
Journal:  ACS Chem Biol       Date:  2020-11-03       Impact factor: 5.100
  1 in total

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