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The Epidermal Growth Factor Receptor (EGFR) L858R mutant is an activating point mutation in the EGFR gene, where arginine (R) is substituted for leucine (L) at amino acid position 858. This mutation leads to constitutive activation of the receptor’s tyrosine kinase activity, promoting oncogenic signaling pathways associated with increased tumor growth and resistance to apoptosis. It is commonly found in non-small cell lung cancer (NSCLC), particularly adenocarcinoma subtypes. Patients with the L858R mutation respond well initially to first-generation tyrosine kinase inhibitors (TKIs), but resistance often develops.
Inhibition of EGFR tyrosine kinase activity
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