Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes
Martin Hügle,
Xavier Lucas,
Gerhard Weitzel,
Dmytro Ostrovskyi,
Bernhard Breit,
Stefan Gerhardt,
Karin Schmidtkunz,
Manfred Jung,
Roland Schüle,
Oliver Einsle,
Stefan Günther,
Daniel Wohlwend
Affiliations
Martin Hügle
Albert-Ludwigs-Universität Freiburg, Institut für Biochemie, Albertstr. 21, D-79104 Freiburg, Germany
Xavier Lucas
College of Life Sciences, Division of Biological Chemistry and Drug Discovery, University of Dundee, James Black Centre, Dow Street, Dundee DD1 5EH, United Kingdom
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 [1,2]. Keywords: Epigenetics, Bromodomains, Drug discovery, X-ray crystallography
