Isoxazole‐Derived Amino Acids are Bromodomain‐Binding Acetyl‐Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3

A range of isoxazole‐containing amino acids was synthesized that displaced 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...

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Udgivet i:Angew Chem Int Ed Engl
Main Authors: Sekirnik (née Measures), Angelina R., Hewings, David S., Theodoulou, Natalie H., Jursins, Lukass, Lewendon, Katie R., Jennings, Laura E., Rooney, Timothy P. C., Heightman, Tom D., Conway, Stuart J.
Format: Artigo
Sprog:Inglês
Udgivet: John Wiley and Sons Inc. 2016
Fag:
Communications
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5089653/
https://ncbi.nlm.nih.gov/pubmed/27264992
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.201602908
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