Interaction between EGFR Mutant with Gefitinib

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Epidermal Growth factor receptros(EGFT) are transmembrane receptor tyrosine kinase that signal critical for cell proliferation. Mutations upon EGFR kinase are one of the most common cause of clustered cell lung cancer, where 40% of the mutation are caused by a mutation presented by L858R. L858R occures when a point substitution at exon 19 replacing leucine by an arginine that lies directly in the activation loop A of the kinase,Arg858 then distructs cell autoinhibitory interactions. Mutation at the active site could cause series of problems such as accelerating catalysis up to 50 fold, overexpression or mutational malignancies in fibriblasts and lung epithelia cells. However there’s a number of tyrosine kinase inhibitors(TKI) that’s currently been developed and studied. Where gefitinib is one of the first selective inhibitors of EGFR developed to target ATP-binding cleft, interrupting signal transition along with an high affinity towards L858R mutation that contains promissing outcomes of drug development.