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Details on Person L861Q, a substitution of leucine 861 with glutamine, is a do...

Class:IdSummation:1181055
_displayNameL861Q, a substitution of leucine 861 with glutamine, is a do...
_timestamp2011-11-19 04:17:58
created[InstanceEdit:1181057] Orlic-Milacic, Marija, 2011-01-27
literatureReference[LiteratureReference:1181011] An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
[LiteratureReference:1181035] Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
modified[InstanceEdit:1996366] Orlic-Milacic, Marija, 2011-11-19
textL861Q, a substitution of leucine 861 with glutamine, is a documented EGFR mutation in the non-small-cell lung cancer (NSCLC). Leu861, encoded by exon 21, localizes to the N-terminal portion of the activation loop (A loop) of the kinase domain of EGFR and together with Leu858 participates in hydrophobic interactions that keep the kinase in the inactive conformation (Zhang et al. 2006). Replacement of Leu861 with glutamine is expected to destabilize the inactive conformation of EGFR and result in constitutive catalytic activity (Zhang et al. 2006). NSCLCs harboring L861Q mutation in EGFR are responsive to small EGFR-specific tyrosine kinase inhibitors from the 4-anilinoquinazoline group gefitinib (Lynch et al. 2004) and are expected to be responsive to the related drug, erlotinib.
(summation)[EntityWithAccessionedSequence:1177542] EGFR L861Q [plasma membrane] [Homo sapiens]
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