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

详细信息    查看全文

• 作者：Martin H&uuml ; gle^a ; Xavier Lucas^b ; Gerhard Weitzel^c ; ¹ ; Dmytro Ostrovskyi^c ; Bernhard Breit^c ; Stefan Gerhardt^a ; Karin Schmidtkunz^d ; Manfred Jung^d ; Roland Sch&uuml ; le^e ; Oliver Einsle^a ; Stefan G&uuml ; nther^f ; Daniel Wohlwend^a ; ^{wohlwend@bio.chemie.uni-freiburg.de" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Epigenetics ; Bromodomains ; Drug discovery ; X-ray crystallography
• 刊名：Data in Brief
• 出版年：2016
• 出版时间：June 2016
• 年：2016
• 卷：7
• 期：Complete
• 页码：1370-1374
• 全文大小：683 K

文摘

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 [1] and [2].