Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains-Reference-Cited by-同舟云学术

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

Published:2013-09-25 Issue:19 Volume:56 Page:7501-7515
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Mirguet Olivier¹,Gosmini Romain¹,Toum Jérôme¹,Clément Catherine A.¹,Barnathan Mélanie¹,Brusq Jean-Marie¹,Mordaunt Jacqueline E.²,Grimes Richard M.²,Crowe Miriam²,Pineau Olivier¹,Ajakane Myriam¹,Daugan Alain¹,Jeffrey Phillip³,Cutler Leanne³,Haynes Andrea C.³,Smithers Nicholas N.⁴,Chung Chun-wa⁵,Bamborough Paul⁵,Uings Iain J.⁴,Lewis Antonia²,Witherington Jason⁴,Parr Nigel⁴,Prinjha Rab K.⁴,Nicodème Edwige¹

Affiliation:

1. Centre de Recherches François Hyafil, GlaxoSmithKline R&D, 25 Avenue du Québec, 91140 Villebon-sur-Yvette, France

2. Screening & Compound Profiling, Molecular Discovery Research, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

3. Quantitative Pharmacology, EMU Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, U.K.

4. Epinova, Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, U.K.

5. Computational & Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm401088k

Reference46 articles.

1. Chromatin Modifications and Their Function

2. Identification and Characterization of BRDT: A Testis-Specific Gene Related to the Bromodomain Genes RING3 andDrosophila fsh

3. The Bromodomain Protein Brd4 Is a Positive Regulatory Component of P-TEFb and Stimulates RNA Polymerase II-Dependent Transcription

4. Recruitment of P-TEFb for Stimulation of Transcriptional Elongation by the Bromodomain Protein Brd4

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