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Preparation data of the bromodomains BRD3(1) BRD3(2) BRD4(1) and BRPF1B and crystallization of BRD4(1)-inhibitor complexes

机译:溴结构域BRD3(1)BRD3(2)BRD4(1)和BRPF1B的制备数据以及BRD4(1)-抑制剂复合物的结晶

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摘要

This article presents detailed purification procedures for the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B. In addition we provide crystallization protocols for apo BRD4(1) and BRD4(1) in complex with numerous inhibitors. The protocols described here were successfully applied to obtain affinity data by isothermal titration calorimetry (ITC) and by differential scanning fluorimetry (DSF) as well as structural characterizations of BRD4(1) inhibitor complexes (PDB codes: PDB: 4LYI, PDB: 4LZS, PDB: 4LYW, PDB: 4LZR, PDB: 4LYS, PDB: 5D24, PDB: 5D25, PDB: 5D26, PDB: 5D3H, PDB: 5D3J, PDB: 5D3L, PDB: 5D3N, PDB: 5D3P, PDB: 5D3R, PDB: 5D3S, PDB: 5D3T). These data have been reported previously and are discussed in more detail elsewhere , .
机译:本文介绍了溴结构域BRD3(1),BRD3(2),BRD4(1)和BRPF1B的详细纯化程序。此外,我们提供了载有多种抑制剂的载脂蛋白BRD4(1)和BRD4(1)的结晶方案。此处描述的协议已成功应用于通过等温滴定量热(ITC)和差示扫描荧光法(DSF)以及BRD4(1)抑制剂复合物的结构表征获得亲和力数据(PDB代码:PDB:4LYI,PDB:4LZS, PDB:4LYW,PDB:4LZR,PDB:4LYS,PDB:5D24,PDB:5D25,PDB:5D26,PDB:5D3H,PDB:5D3J,PDB:5D3L,PDB:5D3N,PDB:5D3P,PDB:5D3R,PDB: 5D3S,PDB:5D3T)。这些数据先前已报道过,并在其他地方进行了详细讨论。

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