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TitleA Small-Molecule Antagonist of HIF2 alpha Is Efficacious in Preclinical Models of Renal Cell Carcinoma.
Journal, issue, pagesCancer Res., Vol. 76, Page 5491-5500, Year 2016
Publish dateSep 12, 2016 (structure data deposition date)
AuthorsWallace, E.M. / Rizzi, J.P. / Han, G. / Wehn, P.M. / Cao, Z. / Du, X. / Cheng, T. / Czerwinski, R.M. / Dixon, D.D. / Goggin, B.S. ...Wallace, E.M. / Rizzi, J.P. / Han, G. / Wehn, P.M. / Cao, Z. / Du, X. / Cheng, T. / Czerwinski, R.M. / Dixon, D.D. / Goggin, B.S. / Grina, J.A. / Halfmann, M.M. / Maddie, M.A. / Olive, S.R. / Schlachter, S.T. / Tan, H. / Wang, B. / Wang, K. / Xie, S. / Xu, R. / Yang, H. / Josey, J.A.
External linksCancer Res. / PubMed:27635045
MethodsX-ray diffraction
Resolution1.85 Å
Structure data

PDB-5tbm:
Crystal structure of PT2385 bound to HIF2a-B*:ARNT-B* complex
Method: X-RAY DIFFRACTION / Resolution: 1.85 Å

Chemicals

ChemComp-79A:
3-{[(1S)-2,2-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / HIF2 inhibitor HIF2 ligand PAS-B hypoxia inducible factor 2 EPAS1

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