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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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Publicado en:Cancer Discov
Autores principales: 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
Lenguaje:Inglês
Publicado: 2015
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Acceso en línea: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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