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, 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 th...

Full description

Bibliographic Details
Main Authors: Conway, S, Sekirnik, A, Hewings, D, Theodoulou, N, Jursins, L, Lewendon, K, Jennings, L, Rooney, T, Heightman, T
Format: Journal article
Published: Wiley 2016