Journal
FUTURE MEDICINAL CHEMISTRY
Volume 14, Issue 17, Pages 1267-1288Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2021-0343
Keywords
drug resistance; EGFR; monoclonal antibodies; signaling pathways; tyrosine kinase inhibitors
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EGFR plays a significant role in cellular processes such as growth, survival, and differentiation. Its deregulation is implicated in various human malignancies, making it an attractive anticancer target. Current therapeutic strategies show some efficacy in inhibiting EGFR, but resistance limits their clinical benefit.
EGFR is a member of the ERBB family. It plays a significant role in cellular processes such as growth, survival and differentiation via the activation of various signaling pathways. EGFR deregulation is implicated in various human malignancies, and therefore EGFR has emerged as an attractive anticancer target. EGFR inhibition using strategies such as tyrosine kinase inhibitors and monoclonal antibodies hinders cellular proliferation and promotes apoptosis in cancer cells in vitro and in vivo. EGFR inhibition by tyrosine kinase inhibitors has been shown to be a better treatment option than chemotherapy for advanced-stage EGFR-driven non-small-cell lung cancer, yet de novo and acquired resistance limits the clinical benefit of these therapeutic molecules. This review discusses the cellular signaling pathways activated by EGFR. Further, current therapeutic strategies to target aberrant EGFR signaling in cancer and mechanisms of resistance to them are highlighted.
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