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
1998
Structure of Human Methionine Aminopeptidase-2 Complexed with Fumagillin
Liu S, Widom J, Kemp C, Crews C, Clardy J. Structure of Human Methionine Aminopeptidase-2 Complexed with Fumagillin. Science 1998, 282: 1324-1327. PMID: 9812898, DOI: 10.1126/science.282.5392.1324.Peer-Reviewed Original ResearchConceptsStructure-based drug designMetAP-2Resolution crystal structureCovalent bondsMethionine aminopeptidase 2Active siteCrystal structurePolar interactionsDrug designThree-dimensional structureExtensive hydrophobicStructural basisMetAP-1Anticancer agentsNew blood vesselsFumagillin analoguesAdditional affinityReactive epoxidesMolecular targetsFumagillinStructureHydrophobicBondsLikely determinantsEpoxides