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BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Jennings LE, Schiedel M, Hewings DS, Picaud S, Laurin CMC, Bruno PA, Bluck JP, Scorah AR, See L, Reynolds JK, Moroglu M, Mistry IN, Hicks A, Guzanov P, Clayton J, Evans CNG, Stazi G, Biggin PC, Mapp AK, Hammond EM, Humphreys PG, Filippakopoulos P, Conway SJ. Jennings LE, et al. Bioorg Med Chem. 2018 Jul 15;26(11):2937-2957. doi: 10.1016/j.bmc.2018.05.003. Epub 2018 May 15. Bioorg Med Chem. 2018. PMID: 29776834 Free article.
Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3.
Sekirnik Née Measures AR, Hewings DS, Theodoulou NH, Jursins L, Lewendon KR, Jennings LE, Rooney TP, Heightman TD, Conway SJ. Sekirnik Née Measures AR, et al. Among authors: jennings le. Angew Chem Int Ed Engl. 2016 Jul 11;55(29):8353-7. doi: 10.1002/anie.201602908. Epub 2016 Jun 6. Angew Chem Int Ed Engl. 2016. PMID: 27264992 Free PMC article.