Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors

Shadrick, WR; Slavish, PJ; Chai, SC; Waddell, B; Connelly, M; Low, JA; Tallant, C; Young, BM; Bharatham, N; Knapp, S; Boyd, VA; Morfouace, M; Roussel, MF; Chen, TS; Lee, RE; Guy, RK; Shelat, AA; Potter, PM

Shelat, AA; Potter, PM (reprint author), St Jude Childrens Res Hosp, Dept Chem Biol & Therapeut, 262 Danny Thomas Pl, Memphis, TN 38105 USA.

BIOORGANIC & MEDICINAL CHEMISTRY, 2018; 26 (1): 25

Abstract

Within the last decade, the Bromodomain and Extra-Terminal domain family (BET) of proteins have emerged as promising drug targets in diverse clinical ......

Full Text Link