Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor TG-101348

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.

SMNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWN
AQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE

0.20 M sodium potassium tartrate, 0.1 M Bis-Tris propane, pH 7.5, 20.0% PEG3350, 10% ethylene glycol, VAPOR DIFFUSION, SITTING DROP, temperature 277K

HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS

bromodomain, bromodomain containing protein 4, JAK2 kinase inhibitor, FLT3 kinase inhibitor, structural genomics, Structural Genomics Consortium, SGC, TRANSCRIPTION-INHIBITOR complex

NPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQ
ECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE