Article
Hsp90 inhibition suppresses mutant EGFR-T790M signaling and overcomes kinase inhibitor resistance.
Cancer research - 15 Jul 2008
Shimamura Takeshi, Li Danan, Ji Hongbin, Haringsma Henry J, Liniker Elizabeth, Borgman Christa L, Lowell April M, Minami Yuko, McNamara Kate, Perera Samanthi A, Zaghlul Sara, Thomas Roman K, Greulich Heidi, Kobayashi Susumu, Chirieac Lucian R, Padera Robert F, Kubo Shigeto, Takahashi Masaya, Tenen Daniel G, Meyerson Matthew, Wong Kwok-Kin, Shapiro Geoffrey I
Abstract excerpt
The epidermal growth factor receptor (EGFR) secondary kinase domain T790M non-small cell lung cancer (NSCLC) mutation enhances receptor catalytic activity and confers resistance to the reversible tyrosine kinase inhibitors gefitinib and erlotinib. Currently, irreversible inhibitors represent the primary approach in clinical use to circumvent resistance. We show that higher concentrations of the irreversible EGFR...
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