Journal article

Development of chemical probes for the bromodomains of BRD7 and BRD9

Abstract:: The bromodomain family of proteins are 'readers' of acetylated lysines of histones, a key mark in the epigenetic code of gene regulation. Without high quality chemical probes with which to study these proteins, their biological function, and potential use in therapeutics, remains unknown. Recently, a number of chemical ligands were reported for the previously unprobed bromodomain proteins BRD7 and BRD9. Herein the development and characterisation of probes against these proteins is detailed, including the preliminary biological activity of BRD7 and BRD9 assessed using these probes. Future studies utilising these chemically-diverse compounds in parallel will allow for a confident assessment of the role of BRD7/9, and give multiple entry points into any subsequent pharmaceutical programs.

Publication status:: Published

Peer review status:: Peer reviewed

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APA Style

Clark, P., Dixon, D., & Brennan, P. (2016). Development of chemical probes for the bromodomains of BRD7 and BRD9. Drug Discovery Today: Technologies, 19, 73–80.

MLA Style

Clark, P., et al. “Development of Chemical Probes for the Bromodomains of BRD7 and BRD9.” Drug Discovery Today: Technologies, vol. 19, Elsevier, 2016, pp. 73–80.

Chicago Style

Clark, P, D Dixon, and P Brennan. 2016. “Development of Chemical Probes for the Bromodomains of BRD7 and BRD9.” Drug Discovery Today: Technologies 19: 73–80.
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Files:: 9 final.pdf

(Preview, Accepted manuscript, pdf, 2.4MB, Terms of use)

Publisher copy:: 10.1016/j.ddtec.2016.05.002

Authors

+ Clark, P More by this author

Institution:: University of Oxford
Division:: MPLS Division
Department:: Chemistry; Organic Chemistry
Role:: Author

+ Dixon, D More by this author

Institution:: University of Oxford
Division:: MPLS Division
Department:: Chemistry; Organic Chemistry
Oxford college:: Wadham College
Role:: Author

+ Brennan, P More by this author

Institution:: University of Oxford
Division:: Medical Sciences Division
Department:: NDM; Target Discovery Institute
Oxford college:: Corpus Christi College
Role:: Author
ORCID:: 0000-0002-8950-7646

Publisher:: Elsevier
Journal:: Drug Discovery Today: Technologies More from this journal
Volume:: 19
Pages:: 73-80
Publication date:: 2016-08-06
DOI:: 10.1016/j.ddtec.2016.05.002
EISSN:: 1740-6749
ISSN:: 1740-6749
Pmid:: 27769361

Language:: English
Keywords:: transcription factors

humans

animals

ligands

protein domains

drug design

chromosomal proteins, non-histone
Pubs id:: pubs:655114
UUID:: uuid:25cf34eb-9a85-46a7-be41-9eed7f0bb09c
Local pid:: pubs:655114
Source identifiers:: 655114
Deposit date:: 2018-05-22

Terms of use

Copyright holder:: © 2016 Elsevier Ltd All rights reserved
Copyright date:: 2016
Notes:: This is the author accepted manuscript following peer review version of the article. The final version is available online from Elsevier at: 10.1016/j.ddtec.2016.05.002

Licence:: CC Attribution-NonCommercial-NoDerivatives (CC BY-NC-ND)

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