2012
Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain
Park JH, Liu Y, Lemmon MA, Radhakrishnan R. Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain. Biochemical Journal 2012, 448: 417-423. PMID: 23101586, PMCID: PMC3507260, DOI: 10.1042/bj20121513.Peer-Reviewed Original ResearchOccupy EGFR
Park JH, Lemmon MA. Occupy EGFR. Cancer Discovery 2012, 2: 398-400. PMID: 22588876, PMCID: PMC3354646, DOI: 10.1158/2159-8290.cd-12-0144.Peer-Reviewed Original ResearchConceptsEpidermal growth factor receptor (EGFR) mutationsNon-small cell lung cancer (NSCLC) tumorsCell lung cancer tumorsDifferent EGFR mutationsTreatment of glioblastomaLung cancer tumorsDistinct receptor conformationsEGFR mutationsReceptor mutationsEGFR inhibitorsCancer tumorsInhibitor efficacyEGFR mutantsEGFR variantsEGFRGlioblastomaDrug selectivityReceptor conformationNew studiesBarkovichErlotinibGefitinibTumors
2008
Mechanism of Activation and Inhibition of the HER4/ErbB4 Kinase
Qiu C, Tarrant MK, Choi SH, Sathyamurthy A, Bose R, Banjade S, Pal A, Bornmann WG, Lemmon MA, Cole PA, Leahy DJ. Mechanism of Activation and Inhibition of the HER4/ErbB4 Kinase. Structure 2008, 16: 460-467. PMID: 18334220, PMCID: PMC2858219, DOI: 10.1016/j.str.2007.12.016.Peer-Reviewed Original ResearchConceptsErbB4 kinaseEGF receptorBa/F3 cellsReceptor tyrosine kinasesMechanism of activationHER4/ErbB4ErbB family membersKinase domainHER2/ErbB2Kinase activationMutagenesis studiesTyrosine kinaseF3 cellsKinaseDimer conformationErbB familyNormal developmentInactive formAsymmetric dimerMammary glandErbB4ActivationFamily members
2006
EGF-independent activation of cell-surface EGF receptors harboring mutations found in gefitinib-sensitive lung cancer
Choi SH, Mendrola JM, Lemmon MA. EGF-independent activation of cell-surface EGF receptors harboring mutations found in gefitinib-sensitive lung cancer. Oncogene 2006, 26: 1567-1576. PMID: 16953218, DOI: 10.1038/sj.onc.1209957.Peer-Reviewed Original ResearchConceptsEpidermal growth factor receptorTyrosine kinase domainKinase domainEGF receptorRecent structural studiesSomatic mutationsCell surface EGF receptorsTyrosine kinase activityAbsence of EGFAutoinhibitory interactionsActivation loopErbB family membersGrowth factor receptorTyrosine phosphorylationEGFR tyrosine kinase domainKinase activityNull backgroundMechanistic basisOncogenic mutationsBiochemical propertiesCell surfaceCell lung carcinoma patientsFactor receptorMutationsLung carcinoma patients