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TitleA Potent, Metabolically Stable Tubulin Inhibitor Targets the Colchicine Binding Site and Overcomes Taxane Resistance.
Journal, issue, pagesCancer Res., Vol. 78, Page 265-277, Year 2018
Publish dateNov 20, 2016 (structure data deposition date)
AuthorsArnst, K.E. / Wang, Y. / Hwang, D.J. / Xue, Y. / Costello, T. / Hamilton, D. / Chen, Q. / Yang, J. / Park, F. / Dalton, J.T. ...Arnst, K.E. / Wang, Y. / Hwang, D.J. / Xue, Y. / Costello, T. / Hamilton, D. / Chen, Q. / Yang, J. / Park, F. / Dalton, J.T. / Miller, D.D. / Li, W.
External linksCancer Res. / PubMed:29180476
MethodsX-ray diffraction
Resolution2.8 Å
Structure data

PDB-5h7o:
Crystal structure of DJ-101 in complex with tubulin protein
Method: X-RAY DIFFRACTION / Resolution: 2.8 Å

Chemicals

ChemComp-GTP:
GUANOSINE-5'-TRIPHOSPHATE / GTP, energy-carrying molecule*YM

ChemComp-MG:
Unknown entry

ChemComp-CA:
Unknown entry

ChemComp-GOL:
GLYCEROL

ChemComp-GDP:
GUANOSINE-5'-DIPHOSPHATE / GDP, energy-carrying molecule*YM

ChemComp-MES:
2-(N-MORPHOLINO)-ETHANESULFONIC ACID / pH buffer*YM

ChemComp-7Q7:
2-(1H-indol-4-yl)-4-(3,4,5-trimethoxyphenyl)-1H-imidazo[4,5-c]pyridine

ChemComp-ACP:
PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER / AMP-PCP, energy-carrying molecule analogue*YM

ChemComp-HOH:
WATER

Source
  • sus scrofa (pig)
  • bos taurus (domestic cattle)
  • rattus norvegicus (Norway rat)
  • gallus gallus (chicken)
KeywordsSTRUCTURAL PROTEIN / DJ-101 / colchicine site tubulin inhibitor / tubulin / taxane resistance

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