2025
Cancer hotspot mutations rewire ERK2 specificity by selective exclusion of docking interactions
Torres Robles J, Stiegler A, Boggon T, Turk B. Cancer hotspot mutations rewire ERK2 specificity by selective exclusion of docking interactions. Journal Of Biological Chemistry 2025, 301: 108348. PMID: 40015635, DOI: 10.1016/j.jbc.2025.108348.Peer-Reviewed Original ResearchShort linear motifsCancer hotspot mutationsLinear motifsERK substratesYeast two-hybrid libraryHotspot mutationsTwo-hybrid libraryCancer-associated mutantsDocking interactionsWild-type ERK2Cancer-associated mutationsDocking motifBinding sequenceKinase ERK2Co-crystal structureMutant formsERK2 mutantsDisordered regionsERK2MotifStructural rationalePeptide bindingMutationsWT kinasePeptide fragments
2008
Disruption of the EGFR E884–R958 ion pair conserved in the human kinome differentially alters signaling and inhibitor sensitivity
Tang Z, Jiang S, Du R, Petri E, El-Telbany A, Chan P, Kijima T, Dietrich S, Matsui K, Kobayashi M, Sasada S, Okamoto N, Suzuki H, Kawahara K, Iwasaki T, Nakagawa K, Kawase I, Christensen J, Hirashima T, Halmos B, Salgia R, Boggon T, Kern J, Ma P. Disruption of the EGFR E884–R958 ion pair conserved in the human kinome differentially alters signaling and inhibitor sensitivity. Oncogene 2008, 28: 518-533. PMID: 19015641, PMCID: PMC2633425, DOI: 10.1038/onc.2008.411.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SubstitutionAMP-Activated Protein Kinase KinasesAnimalsChlorocebus aethiopsCOS CellsErbB ReceptorsErlotinib HydrochlorideFocal Adhesion Kinase 1HumansIndolesLung NeoplasmsMAP Kinase Signaling SystemMitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase 3Mutation, MissensePiperazinesProtein ConformationProtein Kinase InhibitorsProtein Serine-Threonine KinasesProto-Oncogene ProteinsProto-Oncogene Proteins c-kitProto-Oncogene Proteins c-metProto-Oncogene Proteins c-retQuinazolinesReceptors, Growth FactorSulfonamidesConceptsHuman kinomeEpidermal growth factor receptorKinase substrate recognitionInhibitor sensitivityCancer-associated mutationsSystematic bioinformatics analysisTumor suppressor geneSmall molecule inhibitorsSubstrate recognitionProtein kinaseGrowth factor receptorBioinformatics analysisHomologous residuesDownstream signalingSequence analysisLysine residuesKinomeC-lobeConformational changesFamily inhibitorsMutation cataloguesAdjacent residuesMET inhibitor SU11274Factor receptorMutations
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