Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance
Sun N, Ren C, Kong Y, Zhong H, Chen J, Li Y, Zhang J, Zhou Y, Qiu X, Lin H, Song X, Yang X, Jiang B. Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance. European Journal Of Medicinal Chemistry 2020, 193: 112190. PMID: 32179332, DOI: 10.1016/j.ejmech.2020.112190.Peer-Reviewed Original ResearchMeSH KeywordsAnaplastic Lymphoma KinaseAntineoplastic AgentsCarcinoma, Non-Small-Cell LungCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug DevelopmentDrug Resistance, NeoplasmDrug Screening Assays, AntitumorHEK293 CellsHumansLung NeoplasmsMolecular Docking SimulationMolecular StructureProtein Kinase InhibitorsStructure-Activity RelationshipConceptsAnaplastic large cell lymphomaCell lung cancerLung cancerALK proteinNon-small cell lung cancerDrug resistanceSmall cell lung cancerLarge cell lymphomaPotential therapeutic strategyAnti-proliferation abilityCell linesNPM-ALK fusion proteinT cell linesCancer cell linesEML4-ALKCancer regressionTherapeutic strategiesPotential treatmentGrowth inhibition effectInhibitor drugsALK activityCancerCancer resistanceBrigatinibLymphoma