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Identification of kinase inhibitor targets in the lung cancer microenvironment by chemical and phosphoproteomics.


ABSTRACT: A growing number of gene mutations, which are recognized as cancer drivers, can be successfully targeted with drugs. The redundant and dynamic nature of oncogenic signaling networks and complex interactions between cancer cells and the microenvironment, however, can cause drug resistance. While these challenges can be addressed by developing drug combinations or polypharmacology drugs, this benefits greatly from a detailed understanding of the proteome-wide target profiles. Using mass spectrometry-based chemical proteomics, we report the comprehensive characterization of the drug-protein interaction networks for the multikinase inhibitors dasatinib and sunitinib in primary lung cancer tissue specimens derived from patients. We observed in excess of 100 protein kinase targets plus various p

SUBMITTER: Gridling M 

PROVIDER: S-EPMC4221415 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature