The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor-Reference-Cited by-同舟云学术

The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

Published:2020-07-23 Issue:17 Volume:63 Page:9093-9126
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Seal Jonathan T.^ORCID,Atkinson Stephen J.^ORCID,Aylott Helen,Bamborough Paul^ORCID,Chung Chun-wa^ORCID,Copley Royston C. B.,Gordon Laurie,Grandi Paola¹,Gray James R. J.,Harrison Lee A.,Hayhow Thomas G.,Lindon Matthew,Messenger Cassie,Michon Anne-Marie¹,Mitchell Darren,Preston Alex^ORCID,Prinjha Rab K.,Rioja Inmaculada,Taylor Simon¹,Wall Ian D.,Watson Robert J.,Woolven James M.,Demont Emmanuel H.^ORCID

Affiliation:

1. IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

http://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c00796

Reference89 articles.

1. Functions of bromodomain-containing proteins and their roles in homeostasis and cancer

2. Place your BETs: the therapeutic potential of bromodomains

3. Selective inhibition of BET bromodomains