Cellular sensitivity to EGF receptor inhibitors

作者: Stuart Thomson , John D. Haley , Robert Yauch

DOI: 10.1007/978-1-59745-356-1_22

关键词: Protein kinase domainErlotinibReceptorMutationGefitinibKinaseSignal transductionCancer researchCancerMedicine

摘要: The EGFR pathway is a critical signaling regulation cell proliferation and survival. As such, it frequently deregulated in cancer through over expression of both EGF family ligands receptors by mutation components within the pathway. These characteristics have made this axis an attractive target for development molecularly targeted therapies treatment cancer. To date there are numerous small molecule inhibitors antibodies, either already clinical use or late stage trials, that specifically EGFR. achieved great success treating patients generated large amount interest identifying molecular markers predict benefit mechanisms resistance to such treatments. first major breakthrough line research was identification mutations kinase domain, which rendered receptor hypersensitive actions inhibitors. However, rate insufficient explain overall observed with these inhibitors, suggesting wild-type also received some benefit. Subsequently, efforts been identify biomarkers response other than mutational status.

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