Featured Publications
Modular PROTAC Design for the Degradation of Oncogenic BCR‐ABL
Lai AC, Toure M, Hellerschmied D, Salami J, Jaime‐Figueroa S, Ko E, Hines J, Crews CM. Modular PROTAC Design for the Degradation of Oncogenic BCR‐ABL. Angewandte Chemie International Edition 2015, 55: 807-810. PMID: 26593377, PMCID: PMC4733637, DOI: 10.1002/anie.201507634.Peer-Reviewed Original Research
2021
Synthesis of Isoquinolones by Sequential Suzuki Coupling of 2‑Halobenzonitriles with Vinyl Boronate Followed by Cyclization
Jaime-Figueroa S, Bond MJ, Vergara JI, Swartzel JC, Crews CM. Synthesis of Isoquinolones by Sequential Suzuki Coupling of 2‑Halobenzonitriles with Vinyl Boronate Followed by Cyclization. The Journal Of Organic Chemistry 2021, 86: 8479-8488. PMID: 34047555, DOI: 10.1021/acs.joc.1c00472.Peer-Reviewed Original Research
2018
Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships
Burslem GM, Ottis P, Jaime‐Figueroa S, Morgan A, Cromm PM, Toure M, Crews C. Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships. ChemMedChem 2018, 13: 1508-1512. PMID: 29870139, PMCID: PMC6291207, DOI: 10.1002/cmdc.201800271.Peer-Reviewed Original ResearchConceptsOne-pot synthesisIMiD analoguesStructure-activity relationshipsNarrow structure-activity relationshipMultiple purification stepsEfficient synthesisStepwise routePurification stepsSynthesisAnti-proliferative activityRapid accessProtein cereblonAiolos degradationFunctionalizationAnaloguesCompoundsMoleculesDegradationHereinPurificationRouteAffinityCereblon
1999
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: Insights into specificity and potency
Kim K, Myung J, Sin N, Crews C. Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: Insights into specificity and potency. Bioorganic & Medicinal Chemistry Letters 1999, 9: 3335-3340. PMID: 10612595, DOI: 10.1016/s0960-894x(99)00612-5.Peer-Reviewed Original ResearchTowards 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
1998
Eponemycin analogues: syntheses and use as probes of angiogenesis
Sin N, Meng L, Auth H, Crews C. Eponemycin analogues: syntheses and use as probes of angiogenesis. Bioorganic & Medicinal Chemistry 1998, 6: 1209-1217. PMID: 9784862, DOI: 10.1016/s0968-0896(98)00089-3.Peer-Reviewed Original ResearchChemInform Abstract: Towards the Semi‐Synthesis of Didemnin M. Solution and Solid Phase Syntheses of the Pseudotetrapeptide: pGlu‐GlnΨ[COO]Ala‐Pro‐OH.
WEN J, CREWS C. ChemInform Abstract: Towards the Semi‐Synthesis of Didemnin M. Solution and Solid Phase Syntheses of the Pseudotetrapeptide: pGlu‐GlnΨ[COO]Ala‐Pro‐OH. ChemInform 1998, 29: no-no. DOI: 10.1002/chin.199819211.Peer-Reviewed Original ResearchTowards the semi-synthesis of didemnin M. Solution and solid phase synthese of the pseudotetrapeptide: pGlu-Glnψ[COO]Ala-Pro-OH
Wen J, Crews C. Towards the semi-synthesis of didemnin M. Solution and solid phase synthese of the pseudotetrapeptide: pGlu-Glnψ[COO]Ala-Pro-OH. Tetrahedron Letters 1998, 39: 779-782. DOI: 10.1016/s0040-4039(97)10609-8.Peer-Reviewed Original Research