2021
Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC Resistant to Second-Line Antiandrogen Therapy
Lee G, Nagaya N, Desantis J, Madura K, Sabaawy H, Kim W, Vaz R, Cruciani G, Kim I. Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC Resistant to Second-Line Antiandrogen Therapy. Molecular Cancer Therapeutics 2021, 20: 490-499. PMID: 33277442, DOI: 10.1158/1535-7163.mct-20-0417.Peer-Reviewed Original ResearchConceptsCastration-resistant prostate cancerSecond-line antiandrogen therapyAR full lengthAndrogen receptor splice variant 7AR-V7Antiandrogen therapyAndrogen-responsive prostate cancer cellsProstate cancer cellular proliferationHuman prostate cancer cell linesProstate cancer cell linesStandard of careCancer cellular proliferationCellular proliferationPotential therapeutic valueProstate cancer cellsAgents abirateroneCancer cell linesProteolysis Targeting ChimerasMechanisms of resistanceAndrogen receptorAR DNAProstate cancerTumor growthTherapeutic valueAntiproliferative effects
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