Communication

Fragment-based Identification of Hsp90 Inhibitors

  1. John J. Barker Dr.1,
  2. Oliver Barker Dr.1,
  3. Roberto Boggio Dr.2,
  4. Viddhata Chauhan1,
  5. Robert K. Y. Cheng Dr.1,
  6. Vincent Corden1,
  7. Stephen M. Courtney Dr.1,
  8. Neil Edwards1,
  9. Virginie M. Falque Dr.1,
  10. Fulvia Fusar Dr.3,
  11. Mihaly Gardiner Dr.1,
  12. Estelle M. N. Hamelin Dr.1,
  13. Thomas Hesterkamp Dr.1,
  14. Osamu Ichihara Dr.1,
  15. Richard S. Jones Dr.1,
  16. Owen Mather Dr.1,
  17. Ciro Mercurio Dr.3,
  18. Saverio Minucci Dr.4,
  19. Christian A. G. N. Montalbetti Dr.1,
  20. Annett Müller1,
  21. Deepti Patel1,
  22. Banu G. Phillips1,
  23. Mario Varasi Dr.3,
  24. Mark Whittaker Dr.1,
  25. Dirk Winkler1,
  26. Christopher J. Yarnold Dr.1

Article first published online: 19 MAR 2009

DOI: 10.1002/cmdc.200900011

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, pages 963–966, June 8, 2009

Additional Information

How to Cite

Barker, John J., Barker, O., Boggio, R., Chauhan, V., Cheng, R. K. Y., Corden, V., Courtney, Stephen M., Edwards, N., Falque, Virginie M., Fusar, F., Gardiner, M., Hamelin, E. M. N., Hesterkamp, T., Ichihara, O., Jones, Richard S., Mather, O., Mercurio, C., Minucci, S., Montalbetti, C. A. G. N., Müller, A., Patel, D., Phillips, Banu G., Varasi, M., Whittaker, M., Winkler, D. and Yarnold, Christopher J. (2009), Fragment-based Identification of Hsp90 Inhibitors. ChemMedChem, 4: 963–966. doi: 10.1002/cmdc.200900011

Author Information

  1. 1

    Evotec, 114 Milton Park, Abingdon, Oxfordshire, OX10 4SA (UK), Fax: (+44) 1235 86 31 39

  2. 2

    Congenia S.r.l., Genextra Group, Via Adamello 16, 20139 Milan (Italy)

  3. 3

    DAC S.r.l., Genextra Group, Via Adamello 16, 20139 Milan (Italy), Fax: (+39) 025 74303231

  4. 4

    Department of Biomolecular Sciences and Biotechnologies, University of Milan and Department of Experimental Oncology, European Institute of Oncology, Via Adamello 16, 20139 Milan (Italy), Fax: (+39) 029 4375138

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 19 MAR 2009
  3. Manuscript Revised: 6 FEB 2009
  4. Manuscript Received: 12 JAN 2009

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Keywords:

  • fragment-based screening;
  • Hsp90;
  • oximes;
  • structure-based drug design;
  • tetrahydrobenzopyrimidine

Abstract

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Heat shock protein 90 (Hsp90) plays a key role in stress response and protection of the cell against the effects of mutation. Herein we report the identification of an Hsp90 inhibitor identified by fragment screening using a high-concentration biochemical assay, as well as its optimisation by in silico searching coupled with a structure-based drug design (SBDD) approach.

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