Featured Publications
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
Burslem GM, Smith BE, Lai AC, Jaime-Figueroa S, McQuaid DC, Bondeson DP, Toure M, Dong H, Qian Y, Wang J, Crew AP, Hines J, Crews CM. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chemical Biology 2017, 25: 67-77.e3. PMID: 29129716, PMCID: PMC5831399, DOI: 10.1016/j.chembiol.2017.09.009.Peer-Reviewed Original ResearchConceptsReceptor tyrosine kinasesProtein familyProtein degradationTyrosine kinaseDownstream signaling responseTargeted Protein DegradationDevelopment of PROTACsTargeted degradationEndogenous proteinsSignaling responseChimera technologyCell proliferationPROTACsPROTAC technologyKinaseKinase inhibitorsLigand showAdvantages of degradationReceptor tyrosine kinase inhibitorsTyrosine kinase inhibitorsInhibitionDegradationFamilyPowerful toolProteolysis
2021
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
Bond MJ, Crews CM. Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation. RSC Chemical Biology 2021, 2: 725-742. PMID: 34212149, PMCID: PMC8190915, DOI: 10.1039/d1cb00011j.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