Featured Publications
Modular PROTAC Design for the Degradation of Oncogenic BCR‐ABL
Lai AC, Toure M, Hellerschmied D, Salami J, Jaime‐Figueroa S, Ko E, Hines J, Crews CM. Modular PROTAC Design for the Degradation of Oncogenic BCR‐ABL. Angewandte Chemie International Edition 2015, 55: 807-810. PMID: 26593377, PMCID: PMC4733637, DOI: 10.1002/anie.201507634.Peer-Reviewed Original ResearchChemical Genetic Control of Protein Levels: Selective in Vivo Targeted Degradation
Schneekloth JS, Fonseca FN, Koldobskiy M, Mandal A, Deshaies R, Sakamoto K, Crews CM. Chemical Genetic Control of Protein Levels: Selective in Vivo Targeted Degradation. Journal Of The American Chemical Society 2004, 126: 3748-3754. PMID: 15038727, DOI: 10.1021/ja039025z.Peer-Reviewed Original ResearchConceptsGreen fluorescent proteinProtein functionCell biological questionsGenetic model systemUbiquitin-proteasome pathwayChemical knockoutTargeted degradationBiological questionsProtein degradationGenetic strategiesGenetic controlGenetic lossTarget proteinsFluorescent proteinChimeric moleculesCultured cellsFKBP12 ligandsProteinProtein levelsModel systemWestern blotGeneral strategyFunction analysisVivo examplesFluorometric analysis
2024
Regulated induced proximity targeting chimeras—RIPTACs—A heterobifunctional small molecule strategy for cancer selective therapies
Raina K, Forbes C, Stronk R, Rappi J, Eastman K, Zaware N, Yu X, Li H, Bhardwaj A, Gerritz S, Forgione M, Hundt A, King M, Posner Z, Correia A, McGovern A, Puleo D, Chenard R, Mousseau J, Vergara J, Garvin E, Macaluso J, Martin M, Bassoli K, Jones K, Garcia M, Howard K, Yaggi M, Smith L, Chen J, Mayfield A, De Leon C, Hines J, Kayser-Bricker K, Crews C. Regulated induced proximity targeting chimeras—RIPTACs—A heterobifunctional small molecule strategy for cancer selective therapies. Cell Chemical Biology 2024, 31: 1490-1502.e42. PMID: 39116881, PMCID: PMC11371387, DOI: 10.1016/j.chembiol.2024.07.005.Peer-Reviewed Original ResearchProtein-protein interactionsTarget proteinsTernary complexChemical biology studiesExpressed intracellular proteinStable ternary complexAnti-proliferative responseEssential proteinsProtein proximityEffector ligandsIntracellular proteinsCDK inhibitorsTarget-expressing cellsHeterobifunctional small moleculesSmall moleculesCell survivalTumor cellsTherapeutic modalitiesProteinSelective therapySmall molecule strategiesLigandBiological studies
2017
Proteolysis–Targeting Chimeras: Harnessing the Ubiquitin–Proteasome System to Induce Degradation of Specific Target Proteins
Coleman K, Crews C. Proteolysis–Targeting Chimeras: Harnessing the Ubiquitin–Proteasome System to Induce Degradation of Specific Target Proteins. Annual Review Of Cancer Biology 2017, 2: 1-18. DOI: 10.1146/annurev-cancerbio-030617-050430.Peer-Reviewed Original ResearchProteolysis-targeting chimerasSpecific target proteinsUbiquitin-proteasome systemTarget proteinsNew cell biologyCancer Biology Volume 2Accumulation of proteinsProtein homeostasisUndruggable proteinsE3 ubiquitinMammalian cellsCell biologyProteasome complexFinal online publication dateProteinOnline publication dateProteolytic degradationMultistep processCancer cellsProteasome inhibitorsPathological proteinsNovel therapeuticsCentral roleBifunctional moleculesCells
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
1998
Eponemycin analogues: syntheses and use as probes of angiogenesis
Sin N, Meng L, Auth H, Crews C. Eponemycin analogues: syntheses and use as probes of angiogenesis. Bioorganic & Medicinal Chemistry 1998, 6: 1209-1217. PMID: 9784862, DOI: 10.1016/s0968-0896(98)00089-3.Peer-Reviewed Original Research