Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition-Reference-Cited by-同舟云学术

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Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition

Published:2018 Issue:9 Volume:9 Page:2452-2468
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Runcie A. C.¹²³⁴⁵^ORCID,Zengerle M.¹²³⁴⁵,Chan K.-H.¹²³⁴⁵^ORCID,Testa A.¹²³⁴⁵,van Beurden L.¹²³⁴⁵,Baud M. G. J.¹²³⁴⁵^ORCID,Epemolu O.¹²³⁴⁵,Ellis L. C. J.¹²³⁴⁵,Read K. D.¹²³⁴⁵,Coulthard V.⁶⁷⁸⁵,Brien A.⁶⁷⁸⁵,Ciulli A.¹²³⁴⁵^ORCID

Affiliation:

1. Division of Biological Chemistry and Drug Discovery

2. School of Life Sciences

3. University of Dundee

4. Dundee

5. UK

6. Reach Separations Ltd

7. BioCity Nottingham

8. Nottingham

Abstract

Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins.

Funder

Biotechnology and Biological Sciences Research Council

H2020 European Research Council

H2020 Marie Skłodowska-Curie Actions

Wellcome Trust

Medical Research Council

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2018/SC/C7SC02536J

Reference60 articles.

1. Chemical genetics approaches for selective intervention in epigenetics

2. The promise and peril of chemical probes

3. Target validation using chemical probes

4. Allele-Specific Chemical Genetics: Concept, Strategies, and Applications

5. A chemical switch for inhibitor-sensitive alleles of any protein kinase

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