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Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation

Author

Listed:
  • Tea Pemovska

    (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00290 Helsinki, Finland)

  • Eric Johnson

    (La Jolla Laboratories, Pfizer Worldwide Research & Development)

  • Mika Kontro

    (Hematology Research Unit Helsinki, University of Helsinki, and Helsinki University Hospital Comprehensive Cancer Center, 00290 Helsinki, Finland)

  • Gretchen A. Repasky

    (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00290 Helsinki, Finland)

  • Jeffrey Chen

    (La Jolla Laboratories, Pfizer Worldwide Research & Development
    Present address: Wellspring Biosciences LLC, La Jolla, California 92037, USA.)

  • Peter Wells

    (La Jolla Laboratories, Pfizer Worldwide Research & Development)

  • Ciarán N. Cronin

    (La Jolla Laboratories, Pfizer Worldwide Research & Development)

  • Michele McTigue

    (La Jolla Laboratories, Pfizer Worldwide Research & Development)

  • Olli Kallioniemi

    (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00290 Helsinki, Finland)

  • Kimmo Porkka

    (Hematology Research Unit Helsinki, University of Helsinki, and Helsinki University Hospital Comprehensive Cancer Center, 00290 Helsinki, Finland)

  • Brion W. Murray

    (La Jolla Laboratories, Pfizer Worldwide Research & Development)

  • Krister Wennerberg

    (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00290 Helsinki, Finland)

Abstract

A large ex vivo screen of approved and investigational anti-cancer drugs in primary cells derived from CML and ALL patients identifies axitinib, a VEGFR inhibitor approved for the treatment of kidney cancer, as a potent inhibitor of BCR–ABL1(T315I) with unique binding interactions that overcome the gatekeeper resistance mutation, highlighting the potential of repurposing existing drugs for additional cancer types.

Suggested Citation

  • Tea Pemovska & Eric Johnson & Mika Kontro & Gretchen A. Repasky & Jeffrey Chen & Peter Wells & Ciarán N. Cronin & Michele McTigue & Olli Kallioniemi & Kimmo Porkka & Brion W. Murray & Krister Wennerbe, 2015. "Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation," Nature, Nature, vol. 519(7541), pages 102-105, March.
    • Handle: RePEc:nat:nature:v:519:y:2015:i:7541:d:10.1038_nature14119
    DOI: 10.1038/nature14119
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