2023
Design of a mucin-selective protease for targeted degradation of cancer-associated mucins
Pedram K, Shon D, Tender G, Mantuano N, Northey J, Metcalf K, Wisnovsky S, Riley N, Forcina G, Malaker S, Kuo A, George B, Miller C, Casey K, Vilches-Moure J, Ferracane M, Weaver V, Läubli H, Bertozzi C. Design of a mucin-selective protease for targeted degradation of cancer-associated mucins. Nature Biotechnology 2023, 42: 597-607. PMID: 37537499, PMCID: PMC11018308, DOI: 10.1038/s41587-023-01840-6.Peer-Reviewed Original ResearchCancer progressionSpecific protein glycoformsUndruggable proteinsTargeted degradationProtein degradationBreast cancer progressionCell surface bindingSubstrate selectivityCell-type selectivityCell deathGlycan motifsProtein glycoformsDiscrete peptidesCancer cellsProteinCulture modelProteaseTarget cellsTumor growthCancer-associated mucinsCellsMouse modelDegradersGrowthMotifDesign of Class I/IV Bromodomain-Targeting Degraders for Chromatin Remodeling Complexes
Zahid H, Costello J, Li Y, Kimbrough J, Actis M, Rankovic Z, Yan Q, Pomerantz W. Design of Class I/IV Bromodomain-Targeting Degraders for Chromatin Remodeling Complexes. ACS Chemical Biology 2023, 18: 1278-1293. PMID: 37260298, PMCID: PMC10698694, DOI: 10.1021/acschembio.2c00902.Peer-Reviewed Original ResearchConceptsChromatin Remodeling ComplexNon-BET bromodomainsRemodeling complexProtein degradationHeterobifunctional moleculesBET familyProtein targetsPyrimidine base analogsNumber of degradersDegradersOncogenic roleTernary complexExit vectorsWestern blottingProteinFirst exampleClass IChallenging targetComplexesCECR2ChromatinBromodomainsBPTFFamilyNanoBRET
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
2016
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
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