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Structure paper

TitleMacrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 21, Page 3411-3416, Year 2011
Publish dateMar 24, 2011 (structure data deposition date)
AuthorsZapf, C.W. / Bloom, J.D. / McBean, J.L. / Dushin, R.G. / Nittoli, T. / Otteng, M. / Ingalls, C. / Golas, J.M. / Liu, H. / Lucas, J. ...Zapf, C.W. / Bloom, J.D. / McBean, J.L. / Dushin, R.G. / Nittoli, T. / Otteng, M. / Ingalls, C. / Golas, J.M. / Liu, H. / Lucas, J. / Boschelli, F. / Hu, Y. / Vogan, E. / Levin, J.I.
External linksBioorg. Med. Chem. Lett. / PubMed:21515049
MethodsX-ray diffraction
Resolution1.579 Å
Structure data

PDB-3r91:
Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.
Method: X-RAY DIFFRACTION / Resolution: 1.579 Å

Chemicals

ChemComp-06H:
(6S)-4,6,15,15,18-pentamethyl-5,17-dioxo-2,3,4,5,6,7,14,15,16,17-decahydro-1H-12,8-(metheno)[1,4,9]triazacyclotetradecino[9,8-a]indole-9-carboxamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsCHAPERONE/CHAPERONE INHIBITOR / Chaperone / ATP binding domain / ATP-binding / Nucleotide-binding / Phosphoprotein / Stress response / CHAPERONE-CHAPERONE INHIBITOR complex

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