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Structure paper

TitleTriazolopyrimidines Are Microtubule-Stabilizing Agents that Bind the Vinca Inhibitor Site of Tubulin.
Journal, issue, pagesCell Chem Biol, Vol. 24, Page 737-750.e6, Year 2017
Publish dateMar 28, 2017 (structure data deposition date)
AuthorsSaez-Calvo, G. / Sharma, A. / Balaguer, F.A. / Barasoain, I. / Rodriguez-Salarichs, J. / Olieric, N. / Munoz-Hernandez, H. / Berbis, M.A. / Wendeborn, S. / Penalva, M.A. ...Saez-Calvo, G. / Sharma, A. / Balaguer, F.A. / Barasoain, I. / Rodriguez-Salarichs, J. / Olieric, N. / Munoz-Hernandez, H. / Berbis, M.A. / Wendeborn, S. / Penalva, M.A. / Matesanz, R. / Canales, A. / Prota, A.E. / Jimenez-Barbero, J. / Andreu, J.M. / Lamberth, C. / Steinmetz, M.O. / Diaz, J.F.
External linksCell Chem Biol / PubMed:28579361
MethodsX-ray diffraction
Resolution2.394 Å
Structure data

PDB-5njh:
Triazolopyrimidines stabilize microtubules by binding to the vinca inhibitor site of tubulin
Method: X-RAY DIFFRACTION / Resolution: 2.394 Å

Chemicals

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

ChemComp-MG:
Unknown entry

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

ChemComp-8Z8:
5-chloranyl-7-[(1~{R},5~{S})-3-methoxy-8-azabicyclo[3.2.1]octan-8-yl]-6-[2,4,6-tris(fluoranyl)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine

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

ChemComp-HOH:
WATER

Source
  • rattus norvegicus (Norway rat)
  • gallus gallus (chicken)
  • bos taurus (domestic cattle)
KeywordsSTRUCTURAL PROTEIN / Tubulin / microtubules / microtubule targeting agents / antitumoural / resistance to chemotherapy

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