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Characterizing and Overriding the Structural Mechanism of the Quizartinib-resistant FLT3 “Gatekeeper” F691L Mutation with PLX3397

Tyrosine kinase domain mutations are a common cause of acquired clinical resistance to tyrosine kinase inhibitors (TKIs) used to treat cancer, including the FLT3 inhibitor quizartinib. Mutation of kinase “gatekeeper” residues, which control access to an allosteric pocket adjacent to the ATP-binding...

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Detalhes bibliográficos
Publicado no:Cancer Discov
Main Authors: Smith, Catherine C., Zhang, Chao, Lin, Kimberly, Lasater, Elisabeth A., Zhang, Ying, Massi, Evan, Damon, Lauren E., Pendleton, Matthew, Bashir, Ali, Sebra, Robert, Perl, Alexander, Kasarskis, Andrew, Shellooe, Rafe, Tsang, Garson, Carias, Heidi, Powell, Ben, Burton, Elizabeth A., Matusow, Bernice, Zhang, Jiazhong, Spevak, Wayne, Ibrahim, Prabha N., Le, Mai H., Hsu, Henry H., Habets, Gaston, West, Brian L., Bollag, Gideon, Shah, Neil P.
Formato: Artigo
Idioma:Inglês
Publicado em: 2015
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4522415/
https://ncbi.nlm.nih.gov/pubmed/25847190
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1158/2159-8290.CD-15-0060
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