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
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 ResearchMeSH KeywordsBiological ProductsDrug DiscoveryMolecular StructureMultiple MyelomaOligopeptidesProteasome InhibitorsConceptsActive 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