2019
TCF4 induces enzalutamide resistance via neuroendocrine differentiation in prostate cancer
Lee G, Rosenfeld J, Kim W, Kwon Y, Palapattu G, Mehra R, Kim W, Kim I. TCF4 induces enzalutamide resistance via neuroendocrine differentiation in prostate cancer. PLOS ONE 2019, 14: e0213488. PMID: 31536510, PMCID: PMC6752758, DOI: 10.1371/journal.pone.0213488.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBenzamidesBeta CateninCell Line, TumorDisease Models, AnimalDrug Resistance, NeoplasmHumansMaleMiceMice, KnockoutNeuroendocrine CellsNitrilesPhenylthiohydantoinProstatic NeoplasmsProtein BindingProtein TransportTranscription Factor 7-Like 2 ProteinXenograft Model Antitumor AssaysConceptsCastration-resistant prostate cancerEnzalutamide resistanceTranscription factor 4Neuroendocrine differentiationProstate cancerSecond-generation androgen receptor antagonistHuman prostate cancer cell linesLNCaP human prostate cancer cell lineResistant prostate cancerProstate cancer cell linesStandard of careAndrogen receptor antagonistMouse xenograft modelExpression levelsCell linesTCF4 overexpressionCancer cell linesMedian timeClinical benefitReceptor antagonistNeuroendocrine markersMetastatic CaPTreatment resistanceXenograft modelParental cell line
2014
Enzalutamide: looking back at its preclinical discovery
Ha Y, Kim I. Enzalutamide: looking back at its preclinical discovery. Expert Opinion On Drug Discovery 2014, 9: 837-845. PMID: 24820058, DOI: 10.1517/17460441.2014.918947.Peer-Reviewed Original ResearchConceptsCastration-recurrent PCaFirst-line therapyProstate cancerClinical developmentCastration-recurrent prostate cancerStandard first-line therapyAndrogen-AR axisAR agonist activityMetastatic prostate cancerAR nuclear translocationSelective AR modulatorsFurther clinical studiesAndrogen receptor antagonistPre-clinical discoveryDrug clinical developmentSequential therapyOverall survivalTargeted agentsReceptor antagonistClinical studiesPreclinical discoveryNew agentsAR modulatorsAgonist activityFDA approval