Featured Publications
Induced protein degradation: an emerging drug discovery paradigm
Lai AC, Crews CM. Induced protein degradation: an emerging drug discovery paradigm. Nature Reviews Drug Discovery 2016, 16: 101-114. PMID: 27885283, PMCID: PMC5684876, DOI: 10.1038/nrd.2016.211.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsDrug DiscoveryHigh-Throughput Screening AssaysHumansMutant Chimeric ProteinsProtein BindingProteinsProteomicsSmall Molecule LibrariesConceptsProteolysis-targeting chimaerasProtein degradationUndruggable proteomeTarget protein degradationDifferent E3 ligasesInhibitor-based approachE3 ligasesDrug discovery platformProtein targetsProteomeDiscovery platformProtein expressionDrug discovery paradigmInhibition approachCell culturesDiscovery paradigmLigasesExact mechanismDegradationMouse modelDegradersProteinChimaerasPicomolar potency
2010
Targeting the Undruggable Proteome: The Small Molecules of My Dreams
Crews CM. Targeting the Undruggable Proteome: The Small Molecules of My Dreams. Cell Chemical Biology 2010, 17: 551-555. PMID: 20609404, PMCID: PMC2925121, DOI: 10.1016/j.chembiol.2010.05.011.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsDrug DesignGeneticsHigh-Throughput Screening AssaysHumansProteomeSmall Molecule LibrariesConceptsTraditional genetic screensGenetic screenSmall moleculesUndruggable proteomeChemical genetic approachActive small moleculesSmall druglike moleculesSmall molecule librariesAreas of biologyChemical geneticsOrganismal levelDruglike moleculesDrug development effortsGenetic approachesCell biologyPharmaceutical interestBiological processesMolecule librariesPhenotypic changesMoleculesProteomeEarlier compoundsBiologyScreenNew bioassay