2020
Abstract 5509: Breaking the paradox breakers - RAF inhibitor mechanisms
Mendiratta G, McFall T, Stites E. Abstract 5509: Breaking the paradox breakers - RAF inhibitor mechanisms. Cancer Research 2020, 80: 5509-5509. DOI: 10.1158/1538-7445.am2020-5509.Peer-Reviewed Original ResearchSW48 colon cancer cellsMechanism of PAColon cancer cellsParadoxical activationRaf activationAmerican Association for Cancer ResearchATP-competitive inhibitorsDimer stabilityDownstream signalingUpstream mutationsOnco-proteinRafInhibitor mechanismCancer cellsV600 mutationMutationsRegulatory processesDriver mutationsMelanoma cellsSide effectsCombined treatmentPotential PAProteinDrug bindingNo PA
2013
Allosteric Activation of Functionally Asymmetric RAF Kinase Dimers
Hu J, Stites E, Yu H, Germino E, Meharena H, Stork P, Kornev A, Taylor S, Shaw A. Allosteric Activation of Functionally Asymmetric RAF Kinase Dimers. Cell 2013, 154: 1036-1046. PMID: 23993095, PMCID: PMC3844432, DOI: 10.1016/j.cell.2013.07.046.Peer-Reviewed Original ResearchMeSH KeywordsAllosteric RegulationAmino Acid MotifsAmino Acid SequenceAnimalsCell LineDimerizationEnzyme ActivationHumansMiceModels, MolecularMolecular Sequence DataMutationPhosphorylationProtein ConformationProtein KinasesProto-Oncogene Proteins B-rafProto-Oncogene Proteins c-rafRaf KinasesSequence AlignmentTryptophanConceptsN-terminal phosphorylationReceiver kinaseRaf kinaseActivation-loop phosphorylationPhosphorylation of CRAFConstitutively active mutantCis-autophosphorylationRaf activationActive mutantActivated CRAFActive kinaseMechanism of activationKinase activityActive conformationKinasePhosphorylationControl cellsRafCRAFDimerMutantsRasActivityMEKBRAF