Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRα, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

Many clinically validated kinases, such as BCR-ABL, c-Kit, PDGFR, and EGFR, become resistant to adenosine triphosphate-competitive inhibitors through mutation of the so-called gatekeeper amino acid from a threonine to a large hydrophobic amino acid, such as an isoleucine or methionine. We have devel...

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Bibliografische gegevens
Hoofdauteurs: Weisberg, Ellen, Choi, Hwan Geun, Ray, Arghya, Barrett, Rosemary, Zhang, Jianming, Sim, Taebo, Zhou, Wenjun, Seeliger, Markus, Cameron, Michael, Azam, Mohammed, Fletcher, Jonathan A., Debiec-Rychter, Maria, Mayeda, Mark, Moreno, Daisy, Kung, Andrew L., Janne, Pasi Antero, Khosravi-Far, Roya, Melo, Junia V., Manley, Paul W., Adamia, Sophia, Wu, Catherine, Gray, Nathanael, Griffin, James D.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: American Society of Hematology 2010
Onderwerpen:
Myeloid Neoplasia
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2879103/
https://ncbi.nlm.nih.gov/pubmed/20299508
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1182/blood-2009-11-251751
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