Crystal structure of the first bromodomain (BD1) of human BRD4 bound to NC-III-53

Crystal structure of the first bromodomain (BD1) of human BRD4 bound to NC-III-53 Descriptor: Bromodomain-containing protein 4, N-[4-(4-chlorophenoxy)-3-(2-methyl-1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]ethanesulfonamide Authors: Chan, A, Schonbrunn, E. Deposit date: 2021-05-07 Release date: 2022-08-03 Last modified: 2023-10-18 Method: X-RAY DIFFRACTION (1.2 Å) Cite: Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity. J.Med.Chem., 65, 2022人源BRD4的首个溴结构域（Bromodomain，BD1）与NC-III-53结合的晶体结构 描述：含溴结构域蛋白4（Bromodomain-containing protein 4），N-[4-(4-氯苯氧基)-3-(2-甲基-1-氧代-1,2-二氢异喹啉-4-基)苯基]乙磺酰胺 作者：Chan, A、Schonbrunn, E 存放日期：2021-05-07 发布日期：2022-08-03 最后修改日期：2023-10-18 实验方法：X射线衍射（X-RAY DIFFRACTION，分辨率1.2 Å） 引用：《二价BET溴结构域抑制剂通过蛋白质构象可塑性赋予BRDT更强效力与选择性》，J. Med. Chem., 65, 2022