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TitleDiscovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.
Journal, issue, pagesJ. Med. Chem., Vol. 61, Page 6685-6704, Year 2018
Publish dateMay 31, 2018 (structure data deposition date)
AuthorsQin, C. / Hu, Y. / Zhou, B. / Fernandez-Salas, E. / Yang, C.Y. / Liu, L. / McEachern, D. / Przybranowski, S. / Wang, M. / Stuckey, J. ...Qin, C. / Hu, Y. / Zhou, B. / Fernandez-Salas, E. / Yang, C.Y. / Liu, L. / McEachern, D. / Przybranowski, S. / Wang, M. / Stuckey, J. / Meagher, J. / Bai, L. / Chen, Z. / Lin, M. / Yang, J. / Ziazadeh, D.N. / Xu, F. / Hu, J. / Xiang, W. / Huang, L. / Li, S. / Wen, B. / Sun, D. / Wang, S.
External linksJ. Med. Chem. / PubMed:30019901
MethodsX-ray diffraction
Resolution1.47 Å
Structure data

PDB-6dl2:
BRD4 bromodomain 1 in complex with HYB157
Method: X-RAY DIFFRACTION / Resolution: 1.47 Å

Chemicals

ChemComp-GUJ:
3-benzyl-2,9-dimethyl-4H,6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]oxazepine

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / Bromodomain

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