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Structure paper

TitleDevelopment and evaluation of a novel series of Nitroxoline-derived BET inhibitors with antitumor activity in renal cell carcinoma.
Journal, issue, pagesOncogenesis, Vol. 7, Page 83-83, Year 2018
Publish dateJan 20, 2018 (structure data deposition date)
AuthorsChen, W. / Zhang, H. / Chen, Z. / Jiang, H. / Liao, L. / Fan, S. / Xing, J. / Xie, Y. / Chen, S. / Ding, H. ...Chen, W. / Zhang, H. / Chen, Z. / Jiang, H. / Liao, L. / Fan, S. / Xing, J. / Xie, Y. / Chen, S. / Ding, H. / Chen, K. / Luo, C. / Zheng, M. / Yao, Z. / Huang, Y. / Zhang, Y.
External linksOncogenesis / PubMed:30385738
MethodsX-ray diffraction
Resolution1.631 - 1.991 Å
Structure data

PDB-5z5t:
The first bromodomain of BRD4 with compound BDF-2141
Method: X-RAY DIFFRACTION / Resolution: 1.991 Å

PDB-5z5u:
The first bromodomain of BRD4 with compound BDF-2254
Method: X-RAY DIFFRACTION / Resolution: 1.631 Å

PDB-5z5v:
The first bromodomain of BRD4 with compound BDF-1253
Method: X-RAY DIFFRACTION / Resolution: 1.66 Å

Chemicals

ChemComp-96R:
2-amino-4-(1H-imidazol-1-yl)quinolin-8-ol

ChemComp-HOH:
WATER

ChemComp-96U:
2-amino-4-(1H-imidazol-1-yl)quinoline-6,8-diol

ChemComp-96X:
N-{8-hydroxy-4-[(1H-imidazol-1-yl)methyl]quinolin-2-yl}acetamide

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION/INHIBITOR / BRD4 / Inhibitor / Complex / PROTEIN BINDING / TRANSCRIPTION-INHIBITOR complex

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