2007
Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib
Mulloy R, Ferrand A, Kim Y, Sordella R, Bell D, Haber D, Anderson K, Settleman J. Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib. Cancer Research 2007, 67: 2325-2330. PMID: 17332364, DOI: 10.1158/0008-5472.can-06-4293.Peer-Reviewed Original ResearchConceptsEpidermal growth factor receptorEpidermal growth factor receptor mutantMultiple levels in vivoIn vitro kinase assayEpidermal growth factor receptor functionPurified recombinant proteinWild-type epidermal growth factor receptorSensitivity to kinase inhibitionNon-small cell lung cancerCOOH-terminal tyrosineHuman non-small cell lung cancerIncreased sensitivity to gefitinibSensitivity to gefitinibCell lung cancerAutophosphorylation activityGrowth factor receptorCell-based studiesEGFR kinase inhibitorsCytoplasmic domainRecombinant proteinsKinase assayEnzyme functionDownstream effectorsMutantsKinase activity
2000
Insights into the HER-2 Receptor Tyrosine Kinase Mechanism and Substrate Specificity Using a Transient Kinetic Analysis †
Jan A, Johnson E, Diamonti A, Carraway K, Anderson K. Insights into the HER-2 Receptor Tyrosine Kinase Mechanism and Substrate Specificity Using a Transient Kinetic Analysis †. Biochemistry 2000, 39: 9786-9803. PMID: 10933796, DOI: 10.1021/bi9924922.Peer-Reviewed Original ResearchConceptsReceptor tyrosine kinasesRecombinant proteinsTyrosine kinaseSerine/threonine kinaseProtein kinase familyReceptor-like proteinCatalytic mechanismDegenerate peptide libraryStopped-flow fluorescence studiesIntracellular tyrosine kinase domainTyrosine kinase mechanismTyrosine kinase domainState kinetic analysisThreonine kinaseKinase familyCatalytic subunitKinase domainPhosphorylation stateSubstrate specificityProtein modificationNucleotide interactionsKinase mechanismConformational changesTransient kinetic investigationsHER-2/erbB