2022
PROTAC targeted protein degraders: the past is prologue
Békés M, Langley DR, Crews CM. PROTAC targeted protein degraders: the past is prologue. Nature Reviews Drug Discovery 2022, 21: 181-200. PMID: 35042991, PMCID: PMC8765495, DOI: 10.1038/s41573-021-00371-6.Peer-Reviewed Original Research
2021
Targeted protein degradation: A promise for undruggable proteins
Samarasinghe KTG, Crews CM. Targeted protein degradation: A promise for undruggable proteins. Cell Chemical Biology 2021, 28: 934-951. PMID: 34004187, PMCID: PMC8286327, DOI: 10.1016/j.chembiol.2021.04.011.Peer-Reviewed Original ResearchConceptsProteolysis Targeting ChimerasUndruggable proteinsDisease-causing proteinsProtein degradation strategiesProteostasis mechanismsProtein homeostasisTranscription factorsProtein degradationHeterobifunctional moleculesProteinDegradation strategiesDisease initiationBiological effectsProteostasisDegradationPotential therapeutic modalityHomeostasisChimerasCellsAccumulation
2015
Small molecule‐induced catalytic ubiquitination of non‐natural substrates
Bondeson D, Pancevac C, Kruidenier L, Carter P, Churcher I, Crews C. Small molecule‐induced catalytic ubiquitination of non‐natural substrates. The FASEB Journal 2015, 29 DOI: 10.1096/fasebj.29.1_supplement.573.43.Peer-Reviewed Original Research
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