title: Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes.
abstract: 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].
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Biochemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Martin
authors.initials: M
authors.lastname: Hügle
authors.affiliation: College of Life Sciences, Division of Biological Chemistry and Drug Discovery, University of Dundee, James Black Centre, Dow Street, Dundee DD1 5EH, United Kingdom.
authors.forename: Xavier
authors.initials: X
authors.lastname: Lucas
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Organische Chemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Gerhard
authors.initials: G
authors.lastname: Weitzel
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Organische Chemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Dmytro
authors.initials: D
authors.lastname: Ostrovskyi
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Organische Chemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Bernhard
authors.initials: B
authors.lastname: Breit
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Biochemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Gerhardt
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Pharmazeutische Wissenschaften, Albertstr. 25, D-79104 Freiburg, Germany.
authors.forename: Karin
authors.initials: K
authors.lastname: Schmidtkunz
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Pharmazeutische Wissenschaften, Albertstr. 25, D-79104 Freiburg, Germany.
authors.forename: Manfred
authors.initials: M
authors.lastname: Jung
authors.affiliation: Urologische Klinik/Frauenklinik, Klinikum der Universität Freiburg and BIOSS Centre for Biological Signalling Studies, Freiburg, Germany.
authors.forename: Roland
authors.initials: R
authors.lastname: Schüle
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Biochemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Oliver
authors.initials: O
authors.lastname: Einsle
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Pharmazeutische Wissenschaften, Hermann-Herder-Str. 8, D-79104 Freiburg, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Günther
authors.affiliation: Albert-Ludwigs-Universität Freiburg, Institut für Biochemie, Albertstr. 21, D-79104 Freiburg, Germany.
authors.forename: Daniel
authors.initials: D
authors.lastname: Wohlwend
keywords: Bromodomains; Drug discovery; Epigenetics; X-ray crystallography