Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit-Reference-Cited by-同舟云学术

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

Published:2012-11-08 Issue:22 Volume:55 Page:9831-9837
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Fish Paul V.¹,Filippakopoulos Panagis²,Bish Gerwyn¹,Brennan Paul E.²,Bunnage Mark E.¹,Cook Andrew S.¹,Federov Oleg²,Gerstenberger Brian S.³,Jones Hannah⁴,Knapp Stefan²,Marsden Brian²,Nocka Karl⁴,Owen Dafydd R.¹,Philpott Martin²,Picaud Sarah²,Primiano Michael J.⁴,Ralph Michael J.¹,Sciammetta Nunzio¹,Trzupek John D.⁴

Affiliation:

1. Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Ramsgate Road, Sandwich CT13 9NJ, United Kingdom

2. Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, United Kingdom

3. Pfizer Worldwide Medicinal Chemistry, Pfizer Worldwide R&D, Eastern Pont Road, Groton, Connecticut 06340, United States

4. Pfizer Worldwide R&D, 35/200 Cambridgepark Drive, Cambridge, Massachusetts 02140, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm3010515

Reference24 articles.

1. Bromodomains: a new target class for small molecule drug discovery

2. Translating the Histone Code

3. Chromatin Modifications and Their Function