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The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1

Author

Listed:
  • Andrew A. Wylie

    (Novartis Institutes for BioMedical Research)

  • Joseph Schoepfer

    (Novartis Institutes for BioMedical Research)

  • Wolfgang Jahnke

    (Novartis Institutes for BioMedical Research)

  • Sandra W. Cowan-Jacob

    (Novartis Institutes for BioMedical Research)

  • Alice Loo

    (Novartis Institutes for BioMedical Research)

  • Pascal Furet

    (Novartis Institutes for BioMedical Research)

  • Andreas L. Marzinzik

    (Novartis Institutes for BioMedical Research)

  • Xavier Pelle

    (Novartis Institutes for BioMedical Research)

  • Jerry Donovan

    (Novartis Institutes for BioMedical Research)

  • Wenjing Zhu

    (Novartis Institutes for BioMedical Research)

  • Silvia Buonamici

    (Novartis Institutes for BioMedical Research
    † Present addresses: H3 Biomedicine Target Biology, 300 Technology Square, Cambridge, Massachusetts 02139, USA.)

  • A. Quamrul Hassan

    (Novartis Institutes for BioMedical Research)

  • Franco Lombardo

    (Novartis Institutes for BioMedical Research)

  • Varsha Iyer

    (Novartis Institutes for BioMedical Research)

  • Michael Palmer

    (Novartis Institutes for BioMedical Research)

  • Giuliano Berellini

    (Novartis Institutes for BioMedical Research)

  • Stephanie Dodd

    (Novartis Institutes for BioMedical Research)

  • Sanjeev Thohan

    (Novartis Institutes for BioMedical Research)

  • Hans Bitter

    (Novartis Institutes for BioMedical Research)

  • Susan Branford

    (Centre for Cancer Biology, SA Pathology and University of South Australia)

  • David M. Ross

    (Haematology Directorate, SA Pathology)

  • Timothy P. Hughes

    (South Australian Health & Medical Research Institute (SAHMRI), North Terrace)

  • Lilli Petruzzelli

    (Novartis Institutes for BioMedical Research)

  • K. Gary Vanasse

    (Novartis Institutes for BioMedical Research)

  • Markus Warmuth

    (Novartis Institutes for BioMedical Research
    † Present addresses: H3 Biomedicine Target Biology, 300 Technology Square, Cambridge, Massachusetts 02139, USA.)

  • Francesco Hofmann

    (Novartis Institutes for BioMedical Research)

  • Nicholas J. Keen

    (Novartis Institutes for BioMedical Research)

  • William R. Sellers

    (Novartis Institutes for BioMedical Research)

Abstract

The selective allosteric ABL1 inhibitor ABL001 (asciminib) represents a new inhibitory mechanism for BCR–ABL1-driven malignancies, and its efficacy and evolving mechanisms of resistance do not overlap with those of other BCR–ABL1 kinase inhibitors.

Suggested Citation

  • Andrew A. Wylie & Joseph Schoepfer & Wolfgang Jahnke & Sandra W. Cowan-Jacob & Alice Loo & Pascal Furet & Andreas L. Marzinzik & Xavier Pelle & Jerry Donovan & Wenjing Zhu & Silvia Buonamici & A. Quam, 2017. "The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1," Nature, Nature, vol. 543(7647), pages 733-737, March.
    • Handle: RePEc:nat:nature:v:543:y:2017:i:7647:d:10.1038_nature21702
    DOI: 10.1038/nature21702
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    Cited by:

    1. Fanjun Li & Monifa A. Fahie & Kaitlyn M. Gilliam & Ryan Pham & Min Chen, 2022. "Mapping the conformational energy landscape of Abl kinase using ClyA nanopore tweezers," Nature Communications, Nature, vol. 13(1), pages 1-10, December.
    2. Tyler S. Beyett & Ciric To & David E. Heppner & Jaimin K. Rana & Anna M. Schmoker & Jaebong Jang & Dries J. H. Clercq & Gabriel Gomez & David A. Scott & Nathanael S. Gray & Pasi A. Jänne & Michael J. , 2022. "Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors," Nature Communications, Nature, vol. 13(1), pages 1-11, December.

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