And proteins control the structure and function of all the cells that make up your body. Gefitinib and erlotinib are first-technology, reversible EGFR inhibitors. Currently being developed are second-generation irreversible EGFR inhibitors, which inhibit EGFR kinase activity even when the T790M mutation is present. For MET gene amplification, the MET inhibitor PHA has been developed (Engelman, Zejnullahu et al. 2007). Recently, new EGFR inhibitors (WZ4002, WZ3146, and WZ8040) have been reported that suppress the growth of EGFR T790M-containing cell traces by inhibiting phosphorylation (Zhou, Ercan et al. 2009).
L858R mutation causes constitutive activation of the tyrosine kinase of EGFR. Oncogenic mutation of EGFR activates downstream signaling pathways of EGFR, that are implicated in tumor cell growth, proliferation, and survival. This discovery led to the development of the selective EGFR TKIs erlotinib and gefitinib. Inhibition of EGFR by EGFR inhibitors blocks the activity of tyrosine kinase, and hence the activation of … Read MoreRead More »