Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode

Lucas, SCC; Atkinson, SJ; Bamborough, P; Barnett, H; Chung, CW; Gordon, L; Mitchell, DJ; Phillipou, A; Prinjha, RK; Sheppard, RJ; Tomkinson, NCO; Watson, RJ; Demont, EH

Atkinson, SJ (corresponding author), GlaxoSmithKline Med Res Ctr, Epigenet Discovery Performance Unit, Stevenage SG1 2NY, Herts, England.

JOURNAL OF MEDICINAL CHEMISTRY, 2020; 63 (10): 5212

Abstract

Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved as......

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