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
2006
Construction of Highly Substituted Stereodefined Dienes by Cross‐Coupling of α‐Allenic Acetates
Schneekloth J, Pucheault M, Crews C. Construction of Highly Substituted Stereodefined Dienes by Cross‐Coupling of α‐Allenic Acetates. European Journal Of Organic Chemistry 2006, 2007: 40-43. DOI: 10.1002/ejoc.200600721.Peer-Reviewed Original ResearchNatural product chemistryStraightforward reaction conditionsOrganic chemistryProduct chemistryOrganozinc reagentsSubstrate scopeReaction conditionsPalladium precatalystsHigh selectivityZ selectivityCross couplingSelectivityChemistryReactionLigandsDieneInteresting reversalPrecatalystOlefinsReagentsProductsAcetateAssemblyBroad useAppropriate choice
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 acidsSynthesisCompoundsComplexes