2001
Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation
Sakamoto K, Kim K, Kumagai A, Mercurio F, Crews C, Deshaies R. Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation. Proceedings Of The National Academy Of Sciences Of The United States Of America 2001, 98: 8554-8559. PMID: 11438690, PMCID: PMC37474, DOI: 10.1073/pnas.141230798.Peer-Reviewed Original ResearchConceptsSkp1-CullinF-box complexAttachment of ubiquitinUbiquitin-dependent proteolysisMetAP-2Disease-causing proteinsMethionine aminopeptidase 2SCF complexBeta-TRCPConditional inactivationBox complexChimeric moleculesProteinUbiquitinationIntracellular levelsUbiquitinChimeric compoundsAngiogenesis inhibitorsHRT1ComplexesPhosphopeptidesDomainProteolysisEnzymeDegradation
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