2023
Targeted Dephosphorylation of Tau by Phosphorylation Targeting Chimeras (PhosTACs) as a Therapeutic Modality
Hu Z, Chen P, Li W, Douglas T, Hines J, Liu Y, Crews C. Targeted Dephosphorylation of Tau by Phosphorylation Targeting Chimeras (PhosTACs) as a Therapeutic Modality. Journal Of The American Chemical Society 2023, 145: 4045-4055. PMID: 36753634, DOI: 10.1021/jacs.2c11706.Peer-Reviewed Original ResearchProtein tauTau dephosphorylationDisease-modifying therapiesMicrotubule-associated protein tauTau phosphorylation levelsImportant pathological roleTherapeutic modalitiesTau phosphorylationAlzheimer's diseaseTau proteinTherapeutic potentialPathological roleKinase inhibitorsEnhanced downregulationLimited benefitPhosphorylation levelsTauTauopathiesDiseaseCurrent strategiesTau phosphatase
2016
Small‐Molecule PROTACS: New Approaches to Protein Degradation
Toure M, Crews CM. Small‐Molecule PROTACS: New Approaches to Protein Degradation. Angewandte Chemie International Edition 2016, 55: 1966-1973. PMID: 26756721, DOI: 10.1002/anie.201507978.Peer-Reviewed Original ResearchConceptsProteolysis-targeting chimerasProtein degradationCellular quality control machineryQuality control machineryNovel catalytic mechanismInhibitor-based approachDrug target spaceProtein functionControl machineryProtein classesProtein destructionCatalytic mechanismCellular levelActive siteTherapeutic potentialOff-target side effectsMachineryRecent reportsChimerasDegradationRecruitmentTherapeuticsInhibition