DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors

[Image: see text] Drug-resistance acquisition through kinase gate-keeper mutations is a major hurdle in the clinic. Here, we determined the first crystal structures of the human FGFR4 kinase domain (FGFR4K) alone and complexed with ponatinib, a promiscuous type-2 (DFG-out) kinase inhibitor, and an o...

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Detalles Bibliográficos
Autores principales: Huang, Zhifeng, Tan, Li, Wang, Huiyan, Liu, Yang, Blais, Steven, Deng, Jingjing, Neubert, Thomas A., Gray, Nathanael S., Li, Xiaokun, Mohammadi, Moosa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4301177/
https://www.ncbi.nlm.nih.gov/pubmed/25317566
http://dx.doi.org/10.1021/cb500674s

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