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

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 () and Krister Wennerberg ()
Additional contact information
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
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

Nature, 2015, vol. 519, issue 7541, 102-105

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.

Date: 2015
References: Add references at CitEc
Citations:

Downloads: (external link)
https://www.nature.com/articles/nature14119 Abstract (text/html)
Access to the full text of the articles in this series is restricted.

Related works:
This item may be available elsewhere in EconPapers: Search for items with the same title.

Export reference: BibTeX RIS (EndNote, ProCite, RefMan) HTML/Text

Persistent link: https://EconPapers.repec.org/RePEc:nat:nature:v:519:y:2015:i:7541:d:10.1038_nature14119

Ordering information: This journal article can be ordered from
https://www.nature.com/

DOI: 10.1038/nature14119

Access Statistics for this article

Nature is currently edited by Magdalena Skipper

More articles in Nature from Nature
Bibliographic data for series maintained by Sonal Shukla () and Springer Nature Abstracting and Indexing ().