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Isoxazole-derived amino acids are bromodomain-binding acetyl-lysine mimics: incorporation into histone H4 peptides and histone H3

Abstract:

A range of isoxazole-containing amino acids was synthesized, which displace acetyl-lysine-containing peptides from the BAZ2A, BRD4(1), and BRD9 bromodomains. Three of these amino acids were incorporated into a histone H4-mimicking peptide and their affinity for BRD4(1) was assessed. Affinities of the isoxazolecontaining peptides are comparable to those of a hyperacetylated histone H4-mimicking cognate peptide, and demonstrated a dependence on the position at which the unnatural residue was in...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1002/anie.201602908

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Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
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Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry
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Funding agency for:
Sekirnik, AR
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Funding agency for:
Hewings, DS
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Publisher:
Wiley-VCH Verlag Publisher's website
Journal:
Angewandte Chemie International Edition Journal website
Volume:
55
Issue:
29
Pages:
8353–8357
Publication date:
2016-06-06
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
URN:
uuid:002d2984-6031-48dd-8967-b770c2d05ec6
Source identifiers:
622228
Local pid:
pubs:622228

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