Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors-Reference-Cited by-同舟云学术

Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors

Published:2021-03-04 Issue:6 Volume:64 Page:3249-3281
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Aylott Helen E.¹^ORCID,Atkinson Stephen J.¹,Bamborough Paul²^ORCID,Bassil Anna¹,Chung Chun-wa²^ORCID,Gordon Laurie²,Grandi Paola³,Gray James R. J.⁴,Harrison Lee A.¹^ORCID,Hayhow Thomas G.¹,Messenger Cassie²,Mitchell Darren¹,Phillipou Alexander²,Preston Alex¹^ORCID,Prinjha Rab K.¹,Rianjongdee Francesco¹,Rioja Inmaculada¹,Seal Jonathan T.¹^ORCID,Wall Ian D.²,Watson Robert J.¹,Woolven James M.²,Demont Emmanuel H.¹^ORCID

Affiliation:

1. Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

2. Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

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

4. Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, 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/acs.jmedchem.0c02156

Reference77 articles.

1. Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

2. The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs

3. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

4. Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma

5. The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer

Cited by 20 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Targeting bromodomian-containing protein 8 (BRD8): An advanced tool to interrogate BRD8;European Journal of Medicinal Chemistry;2024-03

2. Discovery of a brain-permeable bromodomain and extra terminal domain (BET) inhibitor with selectivity for BD1 for the treatment of multiple sclerosis;European Journal of Medicinal Chemistry;2024-02

3. Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia;Journal of Medicinal Chemistry;2024-01-04

4. BET Bromodomain Inhibitors as an Emerging Class of Anticancer Agents;Handbook of Cancer and Immunology;2023-11-08

5. Selectivity Mechanism of Pyrrolopyridone Analogues Targeting Bromodomain 2 of Bromodomain-Containing Protein 4 from Molecular Dynamics Simulations;ACS Omega;2023-09-06