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 ResearchConceptsProteolysis-targeting chimaerasProtein degradationUndruggable proteomeTarget protein degradationDifferent E3 ligasesInhibitor-based approachE3 ligasesDrug discovery platformProtein targetsProteomeDiscovery platformProtein expressionDrug discovery paradigmInhibition approachCell culturesDiscovery paradigmLigasesExact mechanismDegradationMouse modelDegradersProteinChimaerasPicomolar potency
2021
Electrophilic Screening Platforms for Identifying Novel Covalent Ligands for E3 Ligases
Zheng S, Crews CM. Electrophilic Screening Platforms for Identifying Novel Covalent Ligands for E3 Ligases. Biochemistry 2021, 60: 2367-2370. PMID: 34152723, DOI: 10.1021/acs.biochem.1c00301.Peer-Reviewed Original Research