2018
Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships
Burslem GM, Ottis P, Jaime‐Figueroa S, Morgan A, Cromm PM, Toure M, Crews C. Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships. ChemMedChem 2018, 13: 1508-1512. PMID: 29870139, PMCID: PMC6291207, DOI: 10.1002/cmdc.201800271.Peer-Reviewed Original ResearchMeSH KeywordsAdaptor Proteins, Signal TransducingHumansImmunologic FactorsLenalidomideMultiple MyelomaPeptide HydrolasesStructure-Activity RelationshipThalidomideUbiquitin-Protein LigasesConceptsOne-pot synthesisIMiD analoguesStructure-activity relationshipsNarrow structure-activity relationshipMultiple purification stepsEfficient synthesisStepwise routePurification stepsSynthesisAnti-proliferative activityRapid accessProtein cereblonAiolos degradationFunctionalizationAnaloguesCompoundsMoleculesDegradationHereinPurificationRouteAffinityCereblon
2015
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, Hines J, Winkler JD, Crew AP, Coleman K, Crews CM. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Cell Chemical Biology 2015, 22: 755-763. PMID: 26051217, PMCID: PMC4475452, DOI: 10.1016/j.chembiol.2015.05.009.Peer-Reviewed Original ResearchAcetanilidesAdaptor Proteins, Signal TransducingApoptosisAzepinesCell Cycle ProteinsCell Line, TumorCell ProliferationHeterocyclic Compounds, 3-RingHumansNuclear ProteinsPeptide HydrolasesProto-Oncogene Proteins c-mycSignal TransductionThalidomideTranscription FactorsTriazolesUbiquitin-Protein Ligases