A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain-Reference-Cited by-同舟云学术

登录注册会员服务联系我们

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

Published:2016 Issue:3 Volume:7 Page:2322-2330
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Cox Oakley B.¹²³⁴⁵,Krojer Tobias¹²³⁴,Collins Patrick⁶⁷⁸⁴,Monteiro Octovia¹²³⁴⁵,Talon Romain¹²³⁴,Bradley Anthony¹²³⁴,Fedorov Oleg¹²³⁴⁵,Amin Jahangir⁹¹⁰¹¹¹²⁴,Marsden Brian D.¹²³⁴¹³,Spencer John⁹¹⁰¹¹¹²⁴^ORCID,von Delft Frank¹²³⁴⁶,Brennan Paul E.¹²³⁴⁵^ORCID

Affiliation:

1. Structural Genomics Consortium (SGC)

2. University of Oxford

3. Oxford OX3 7DQ

4. UK

5. Target Discovery Institute (TDI)

6. Diamond Light Source (DLS)

7. Harwell Science and Innovation Campus

8. Didcot

9. Department of Chemistry

10. School of Life Sciences

11. University of Sussex

12. Brighton

13. Kennedy Institute of Rheumatology

Abstract

High concentration crystal soaking of poised fragments and one-step elaboration identified compound 17 as an inhibitor of the PHIP(2) bromodomain.

Funder

Takeda Pharmaceutical Company

Novartis

Merck

Janssen Pharmaceuticals

European Commission

Bayer

Worldwide Cancer Research

Wellcome Trust

Engineering and Physical Sciences Research Council

AbbVie

Boehringer Ingelheim

Canada Foundation for Innovation

Genome Canada

Ontario Ministry of Economic Development and Innovation

Pfizer

Fundação de Amparo à Pesquisa do Estado de São Paulo

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2016/SC/C5SC03115J

Reference42 articles.

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

2. Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions

3. Selective inhibition of BET bromodomains

4. Suppression of inflammation by a synthetic histone mimic

5. The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor

Cited by 119 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. Regulation of inositol 5-phosphatase activity by the C2 domain of SHIP1 and SHIP2;Structure;2024-02

2. Fragment-based screening targeting an open form of the SARS-CoV-2 main protease binding pocket;Acta Crystallographica Section D Structural Biology;2024-01-30

3. Fragment library screening by X-ray crystallography and binding site analysis on thioredoxin glutathione reductase of Schistosoma mansoni;Scientific Reports;2024-01-18

4. Targeting the Main Protease (M^pro, nsp5) by Growth of Fragment Scaffolds Exploiting Structure-Based Methodologies;ACS Chemical Biology;2024-01-17

5. PDBe CCDUtils: an RDKit-based toolkit for handling and analysing small molecules in the Protein Data Bank;Journal of Cheminformatics;2023-12-02

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线，采集、加工和组织学术论文而形成的新型学术文献查询和分析系统，可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容，当前同舟云学术共收录了国内外主流学术期刊6万余种，收集的期刊论文及会议论文总量共计约1.5亿篇，并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询！咨询电话：010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号京ICP备18003416号-3