Featured Publications
Catalytic in vivo protein knockdown by small-molecule PROTACs
Bondeson DP, Mares A, Smith IE, Ko E, Campos S, Miah AH, Mulholland KE, Routly N, Buckley DL, Gustafson JL, Zinn N, Grandi P, Shimamura S, Bergamini G, Faelth-Savitski M, Bantscheff M, Cox C, Gordon DA, Willard RR, Flanagan JJ, Casillas LN, Votta BJ, den Besten W, Famm K, Kruidenier L, Carter PS, Harling JD, Churcher I, Crews CM. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nature Chemical Biology 2015, 11: 611-617. PMID: 26075522, PMCID: PMC4629852, DOI: 10.1038/nchembio.1858.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAntineoplastic AgentsBinding SitesBiocatalysisBreast NeoplasmsFemaleHumansMCF-7 CellsMiceModels, MolecularMolecular Targeted TherapyNeoplasm ProteinsNeoplasm TransplantationProteasome Endopeptidase ComplexProtein BindingProteolysisReceptor-Interacting Protein Serine-Threonine Kinase 2Receptors, EstrogenSmall Molecule LibrariesUbiquitinUbiquitinationVon Hippel-Lindau Tumor Suppressor Protein
2001
Cells adapted to the proteasome inhibitor 4-hydroxy- 5-iodo-3-nitrophenylacetyl-Leu-Leu-leucinal-vinyl sulfone require enzymatically active proteasomes for continued survival
Princiotta M, Schubert U, Chen W, Bennink J, Myung J, Crews C, Yewdell J. Cells adapted to the proteasome inhibitor 4-hydroxy- 5-iodo-3-nitrophenylacetyl-Leu-Leu-leucinal-vinyl sulfone require enzymatically active proteasomes for continued survival. Proceedings Of The National Academy Of Sciences Of The United States Of America 2001, 98: 513-518. PMID: 11149939, PMCID: PMC14618, DOI: 10.1073/pnas.98.2.513.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid Chloromethyl KetonesAminopeptidasesAnimalsAntigen PresentationAntigensBoronic AcidsBortezomibCD8-Positive T-LymphocytesCell SurvivalCysteine EndopeptidasesDipeptidyl-Peptidases and Tripeptidyl-PeptidasesDrug ResistanceEndopeptidasesEnzyme ActivationH-2 AntigensLeupeptinsLymphoma, T-CellMiceMultienzyme ComplexesNeoplasm ProteinsOligopeptidesPeptide FragmentsPhenolsProtease InhibitorsProteasome Endopeptidase ComplexProtein Processing, Post-TranslationalPyrazinesSelection, GeneticSerine EndopeptidasesSulfonesThymus NeoplasmsTumor Cells, CulturedTumor Suppressor Protein p53TyramineUbiquitinsConceptsII activityLarge proteolytic complexSpecific proteasome inhibitorInhibitor 4Degradation of p53Ala-AlaProteolytic complexPolyubiquitinated proteinsLeu-LeuProteolytic functionActive proteasomesPrimary proteaseProperties of cellsProteolytic systemProteasomeSpecific inhibitorMajor histocompatibility complexPhe-chloromethylketoneProteasome inhibitors