The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1

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. Quamrul Hassan, Franco Lombardo, Varsha Iyer, Michael Palmer, Giuliano Berellini, Stephanie Dodd, Sanjeev Thohan, Hans Bitter, Susan Branford, David M. Ross, Timothy P. Hughes, Lilli Petruzzelli, K. Gary Vanasse, Markus Warmuth, Francesco Hofmann, Nicholas J. Keen and William R. Sellers
Additional contact information
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
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
Francesco Hofmann: Novartis Institutes for BioMedical Research
Nicholas J. Keen: Novartis Institutes for BioMedical Research
William R. Sellers: Novartis Institutes for BioMedical Research

Nature, 2017, vol. 543, issue 7647, 733-737

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.

Date: 2017
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DOI: 10.1038/nature21702

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