Chemical proteomics uncovers EPHA2 as a mechanism of acquired resistance to small molecule EGFR kinase inhibition.

Data from ProteomeXchange, PXD ID: PXD001333. File: 000249_D01_P001442_B00_A00_R1.mzml. Published as part of J Proteome Res. 2015 May 12 . From the Abstract: {{i}} ... Here, we describe a chemical proteomic approach comprising kinase affinity purification (kinobeads) and quantitative mass spectrometry for the identification of kinase inhibitor resistance mechanisms in cancer cells. We identified the previously described amplification of MET and found EPHA2 to be more than 10-fold overexpressed (p<0.001) in gefitinib resistant HCC827 cells suggesting a potential role in developing resistance. siRNA mediated EPHA2 knock-down or treating cells with the multi-kinase inhibitor dasatinib restored sensitivity to gefitinib ... {{/i}}