2013
From epoxomicin to carfilzomib : chemistry, biology, and medical outcomes
Kim KB, Crews CM. From epoxomicin to carfilzomib : chemistry, biology, and medical outcomes. Natural Product Reports 2013, 30: 600-604. PMID: 23575525, PMCID: PMC3815659, DOI: 10.1039/c3np20126k.Peer-Reviewed Original ResearchConceptsActive natural productsNatural productsNatural product-based drug discoveryAnti-tumor natural productParent lead compoundRational drug designUnprecedented selectivityHigh-throughput screeningPeptide structureMolecular probesImproved activityDrug designLead compoundsDrug discoveryPharmacophoreEpoxyketonesChemistryProductsSelectivityCompoundsTherapeutic agentsBiological processesDiscoveryScaffoldsBristol-Myers Squibb
2001
The ubiquitin‐proteasome pathway and proteasome inhibitors
Myung J, Kim K, Crews C. The ubiquitin‐proteasome pathway and proteasome inhibitors. Medicinal Research Reviews 2001, 21: 245-273. PMID: 11410931, PMCID: PMC2556558, DOI: 10.1002/med.1009.Peer-Reviewed Original ResearchConceptsUbiquitin-proteasome pathwayComplex biochemical machineryHuman diseasesDiverse cellular processesImportant cellular substratesMajor cellular networksCellular processesBiochemical machineryProtein degradationNatural proteasome inhibitorsCellular substratesCentral playerIntracellular processesMode of actionProteasome inhibitorsPathwayMolecular probesInhibitorsPotential therapeutic agentProteasomeImportant componentMachineryRegulationTherapeutic agents
1999
Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide α', β'-epoxyketones
Elofsson M, Splittgerber U, Myung J, Mohan R, Crews C. Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide α', β'-epoxyketones. Cell Chemical Biology 1999, 6: 811-822. PMID: 10574782, DOI: 10.1016/s1074-5521(99)80128-8.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAortaCattleCell DivisionCells, CulturedChymotrypsinCysteine EndopeptidasesCysteine Proteinase InhibitorsDrug DesignEndothelium, VascularEpoxy CompoundsGlutamatesIndicators and ReagentsIrritantsKineticsMacromolecular SubstancesMiceMolecular ConformationMultienzyme ComplexesPeptidesProteasome Endopeptidase ComplexTrypsinConceptsCatalytic activityMolecular probesAcetylated peptidesExcellent selectivityPotent proteasome inhibitorVivo anti-inflammatory activityMost compoundsMajor catalytic activityChymotrypsin-like activityPeptide αAromatic amino acidsEpoxyketonesAminoP2-P4Multicatalytic protease complexPeptidesAnti-inflammatory activitySelectivityProbeLarge multicatalytic protease complexesProteasome inhibitorsAmino acidsSynthesisCompoundsComplexesChemical genetics: exploring and controlling cellular processes with chemical probes
Crews C, Splittgerber U. Chemical genetics: exploring and controlling cellular processes with chemical probes. Trends In Biochemical Sciences 1999, 24: 317-320. PMID: 10431176, DOI: 10.1016/s0968-0004(99)01425-5.Peer-Reviewed Original Research