Article
Biophysical characterization of drug-resistant mutants of fibroblast growth factor receptor 1.
Genes to cells : devoted to molecular & cellular mechanisms - 1 Oct 2016
Yoza Kaito, Himeno Rika, Amano Shinjiro, Kobashigawa Yoshihiro, Amemiya Shun, Fukuda Natsuki, Kumeta Hiroyuki, Morioka Hiroshi, Inagaki Fuyuhiko
Abstract excerpt
Over-expression and aberrant activation of tyrosine kinases occur frequently in human cancers. Various tyrosine kinase inhibitors (TKIs) are under clinical use, but acquisition of resistance to these drugs is a major problem. Here, we studied the interaction between two drug-resistant mutants of fibroblast growth factor receptor 1 (FGFR1), N546K and V561M, and four ATP-competitive inhibitors, ponatinib,...
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