2024
EGFR targeting PhosTACs as a dual inhibitory approach reveals differential downstream signaling
Hu Z, Chen P, Li W, Krone M, Zheng S, Saarbach J, Velasco I, Hines J, Liu Y, Crews C. EGFR targeting PhosTACs as a dual inhibitory approach reveals differential downstream signaling. Science Advances 2024, 10: eadj7251. PMID: 38536914, PMCID: PMC10971414, DOI: 10.1126/sciadv.adj7251.Peer-Reviewed Original ResearchConceptsInhibit cancer cell viabilityProteome-wide levelCancer cell viabilityDifferential signaling pathwaysPhosphoproteomic approachTyrosine dephosphorylationProtein dephosphorylationSignal transductionActivating dephosphorylationInduce apoptosisReceptor tyrosine kinase inhibitorsRTK activationSignaling pathwayInhibition of kinasesDephosphorylationEpidermal growth factor receptorGrowth factor receptorCell viabilityFactor receptorInhibitory approachesTyrosineTyrosine kinase inhibitorsInhibitory effectInhibitory potentialKinase inhibitors
2013
Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs
Hines J, Gough JD, Corson TW, Crews CM. Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs. Proceedings Of The National Academy Of Sciences Of The United States Of America 2013, 110: 8942-8947. PMID: 23674677, PMCID: PMC3670320, DOI: 10.1073/pnas.1217206110.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceAnalysis of VarianceAnimalsChromatography, High Pressure LiquidEnzyme ActivationFemaleGene Knockdown TechniquesHumansImmunoblottingMCF-7 CellsMiceMolecular Sequence DataMolecular StructurePC12 CellsPhosphatidylinositol 3-KinasesPhosphorylationProtein Processing, Post-TranslationalProteolysisRatsReceptor Protein-Tyrosine KinasesReceptor, ErbB-3Receptor, Fibroblast Growth Factor, Type 2Receptor, trkASignal TransductionStreptavidinVon Hippel-Lindau Tumor Suppressor ProteinConceptsGrowth factor receptorProtein knockdownFibroblast growth factor receptor substrateVon Hippel-Lindau proteinSpecific receptor tyrosine kinasesKinase-mediated phosphorylationReceptor tyrosine kinase pathwaysFactor receptorKinase signal pathwayTyrosine kinase activationReceptor tyrosine kinasesTyrosine kinase pathwayConditional degradationPhosphorylation sequenceKinase pathwayReceptor substrateKinase activationNucleic acid-based strategiesLindau proteinTarget protein knockdownSpecific proteinsTyrosine kinaseCell-type selectivityNerve growth factor receptorKnockdown