Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors (Cell Chemical Biology)

Niessen et al. explore the proteome-wide reactivity of third-generation T790M-EGFR inhibitors in human cancer cells and animal models through the development and application of chemical probes and quantitative mass spectrometry-based proteomic methods. These studies highlight the importance of performing global analyses of drug action in living systems to identify targets and off-targets that may affect efficacy and safety.