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
2013
Mechanism of pro‐tumorigenic effect of BMP‐6: Neovascularization involving tumor‐associated macrophages and IL‐1α
Kwon S, Lee G, Lee J, Iwakura Y, Kim W, Kim I. Mechanism of pro‐tumorigenic effect of BMP‐6: Neovascularization involving tumor‐associated macrophages and IL‐1α. The Prostate 2013, 74: 121-133. PMID: 24185914, DOI: 10.1002/pros.22734.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBone Morphogenetic Protein 6CarcinogenesisCell DifferentiationCell Line, TumorCell ProliferationCoculture TechniquesEndothelium, VascularHumansInterleukin-1alphaMacrophagesMaleMiceMice, Inbred C57BLMice, KnockoutNeovascularization, PathologicNF-kappa BProstatic NeoplasmsSignal TransductionSmad1 ProteinConceptsBone morphogenetic protein 6Prostate cancer growthTumor-associated macrophagesIL-1APro-tumorigenic effectsCancer growthHuman prostate cancer cell linesHuman prostate cancer tissuesLNCaP human prostate cancer cell lineProstate cancer cell linesTube formationProstate cancer tissuesTHP-1 cellsEndothelial tube formationCancer cell linesIL-1αProstate cancerKnockout miceCD11b-DTRCancer tissuesTumor growthNF-kB1Endothelial cellsMacrophagesConditioned media
2006
Expression of estrogen receptors‐α and ‐β in bladder cancer cell lines and human bladder tumor tissue
Shen S, Smith C, Hsieh J, Yu J, Kim I, Jian W, Sonpavde, Ayala G, Younes M, Lerner S. Expression of estrogen receptors‐α and ‐β in bladder cancer cell lines and human bladder tumor tissue. Cancer 2006, 106: 2610-2616. PMID: 16700038, DOI: 10.1002/cncr.21945.Peer-Reviewed Original ResearchMeSH KeywordsAntineoplastic AgentsBlotting, WesternCarcinoma, Transitional CellCell Line, TumorCell ProliferationEstradiolEstrogen Receptor alphaEstrogen Receptor betaFulvestrantGene Expression ProfilingGene Expression Regulation, NeoplasticHumansImmunohistochemistryMicroarray AnalysisNeoplasm StagingRaloxifene HydrochlorideReverse Transcriptase Polymerase Chain ReactionRNA, MessengerTamoxifenUrinary Bladder NeoplasmsConceptsBladder cancer cell linesExpression of ERbetaCancer cell linesERbeta expressionHuman bladder cancerBladder cancer cellsBladder cancerEstrogen receptorWestern blot analysisT4 tumorsCell linesMetastatic transitional cell carcinomaMuscle-invasive bladder cancerER-alpha mRNA levelsT3/T4 tumorsHuman bladder tumor tissuesRT4 cellsBladder cancer cell growthLevels of ERalphaGrade 3 tumorsCancer cellsInvasive bladder cancerTa/T1Transitional cell carcinomaEffects of estradiol
2004
Restoration of Bone Morphogenetic Protein Receptor Type II Expression Leads to a Decreased Rate of Tumor Growth in Bladder Transitional Cell Carcinoma Cell Line TSU-Pr1
Kim I, Lee D, Lee D, Kim W, Kim M, Morton R, Lerner S, Kim S. Restoration of Bone Morphogenetic Protein Receptor Type II Expression Leads to a Decreased Rate of Tumor Growth in Bladder Transitional Cell Carcinoma Cell Line TSU-Pr1. Cancer Research 2004, 64: 7355-7360. PMID: 15492256, DOI: 10.1158/0008-5472.can-04-0154.Peer-Reviewed Original ResearchConceptsTSU-Pr1Cell line TSU-Pr1BMP-RIITumor growthBladder transitional cell carcinoma cellsHuman bladder cancer cell linesCell linesTransitional cell carcinoma cellsBladder cancer cell linesBone morphogenetic protein receptor type II (BMPR2) expressionBone morphogenetic proteinTSU-Pr1 cellsBladder TCC tissuesGrowth inhibitory effectsCancer cell linesBladder specimensType II expressionBladder TCCTumor gradeTransitional epitheliumClinical observationsTCC tissuesMalignant cellsSignificant associationBMP-RIALoss of expression of bone morphogenetic protein receptor type II in human prostate cancer cells
Kim I, Lee D, Lee D, Ahn H, Kim M, Kim S, Morton R. Loss of expression of bone morphogenetic protein receptor type II in human prostate cancer cells. Oncogene 2004, 23: 7651-7659. PMID: 15354178, DOI: 10.1038/sj.onc.1207924.Peer-Reviewed Original ResearchConceptsBone morphogenetic proteinProstate cancer cellsHuman prostate cancer cellsLoss of expressionProstate cancer patientsBMP-RIICancer patientsGleason scoreBMP receptor type IABone morphogenetic protein receptor type IICancer cellsSignificant associationHuman prostate cancer cell linesBiochemical recurrence-free rateExpression of BMPRsRecurrence-free rateProstate cancer cell linesCell linesTumor growth rateReceptor type IIParental cell lineCancer cell linesMorphogenetic proteinsClinical stagePrognostic value735: Differential Expression of Estrogen Receptor α and β in Bladder Cancer Cell Lines and Human Bladder Tumor Tissue
Shen S, Yu J, Kim I, Jian W, Matsumoto K, Kim M, Sonpavde G, Smith C, Ayala G, Younes M, Lerner S. 735: Differential Expression of Estrogen Receptor α and β in Bladder Cancer Cell Lines and Human Bladder Tumor Tissue. Journal Of Urology 2004, 171: 195. DOI: 10.1016/s0022-5347(18)37984-9.Peer-Reviewed Original Research
2002
Raloxifene, a mixed estrogen agonist/antagonist, induces apoptosis in androgen-independent human prostate cancer cell lines.
Kim I, Kim B, Seong D, Lee D, Seo J, Hong Y, Kim H, Morton R, Kim S. Raloxifene, a mixed estrogen agonist/antagonist, induces apoptosis in androgen-independent human prostate cancer cell lines. Cancer Research 2002, 62: 5365-9. PMID: 12235008.Peer-Reviewed Original ResearchConceptsAndrogen-independent human prostate cancer cell linesMixed estrogen agonist/antagonistProstate cancer cell linesHuman prostate cancer cell linesEstrogen agonist/antagonistAgonists/antagonistsCancer cell linesER betaER alphaCell linesDU145 cellsSelective estrogen receptor modulatorsEffects of raloxifeneEstrogen receptor modulatorsPC3M cellsDose-dependent mannerCell deathM raloxifeneWestern blot analysisTime-dependent mannerRaloxifene treatmentReceptor modulatorsBreast cancerPan-caspase inhibitor zVADRaloxifeneRaloxifene, a Mixed Estrogen Agonist/Antagonist, Induces Apoptosis through Cleavage of BAD in TSU-PR1 Human Cancer Cells*
Kim H, Kim B, Kim I, Mamura M, Do Hwan Seong, Jang J, Kim S. Raloxifene, a Mixed Estrogen Agonist/Antagonist, Induces Apoptosis through Cleavage of BAD in TSU-PR1 Human Cancer Cells*. Journal Of Biological Chemistry 2002, 277: 32510-32515. PMID: 12084714, DOI: 10.1074/jbc.m202852200.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid Chloromethyl KetonesAntineoplastic AgentsApoptosisBcl-Associated Death ProteinBcl-X ProteinCarrier ProteinsCaspase 3CaspasesCell DivisionCell MembraneCell NucleusCycloheximideCytochrome c GroupDNA FragmentationDose-Response Relationship, DrugEstrogen Receptor ModulatorsHumansIn Situ Nick-End LabelingMembrane PotentialsMitochondriaPhosphorylationProtein BindingProtein Synthesis InhibitorsProto-Oncogene Proteins c-bcl-2Raloxifene HydrochlorideRetroviridaeTime FactorsTumor Cells, CulturedUrinary Bladder NeoplasmsConceptsMixed estrogen agonist/antagonistTSU-Pr1 cell linesEstrogen agonist/antagonistTSU-Pr1 cellsAgonists/antagonistsCell linesSelective estrogen receptor modulatorsHuman bladder transitional cell carcinoma cell lineEffects of raloxifeneTransitional cell carcinoma cell linesProstate cancer cell linesEstrogen receptor modulatorsCell carcinoma cell linesEstrogen receptor betaHuman bladder cancerDose-dependent mannerEvidence of apoptosisCancer cell linesRaloxifene treatmentCarcinoma cell linesBladder cancerReceptor modulatorsBreast cancerHuman cancer cellsRaloxifene
1998
The Conventional Transforming Growth Factor-β (TGF-β) Receptor Type I Is Not Required for TGF-β1 Signaling in a Human Prostate Cancer Cell Line, LNCaP
Kim I, Zelner D, Lee C. The Conventional Transforming Growth Factor-β (TGF-β) Receptor Type I Is Not Required for TGF-β1 Signaling in a Human Prostate Cancer Cell Line, LNCaP. Experimental Cell Research 1998, 241: 151-160. PMID: 9633523, DOI: 10.1006/excr.1998.4034.Peer-Reviewed Original ResearchMeSH KeywordsActivin Receptors, Type IDihydrotestosteroneGene ExpressionHumansMaleProstatic NeoplasmsProtein Serine-Threonine KinasesReceptor, Transforming Growth Factor-beta Type IReceptor, Transforming Growth Factor-beta Type IIReceptors, Transforming Growth Factor betaRNA, MessengerSensitivity and SpecificitySignal TransductionTransforming Growth Factor betaTumor Cells, CulturedConceptsHuman prostate cancer cell linesCompetitive quantitative RT-PCRProstate cancer cell linesType II receptorLNCaP cellsII receptorsWestern blot analysisQuantitative RT-PCRCancer cell linesTGF-beta signalingALK-5RT-PCRALK-1Androgen-responsive human prostate cancer cell lineGrowth factor-β receptor type IType II receptor mRNAReceptor type IConcentrations of dihydrotestosteroneTGF-β1 signalingCell linesBlot analysisType INM dihydrotestosteroneReceptor mRNADihydrotestosterone
1996
Transforming growth factor-beta1 is a mediator of androgen-regulated growth arrest in an androgen-responsive prostatic cancer cell line, LNCaP
Kim I, Kim J, Zelner D, Ahn H, Sensibar J, Lee C. Transforming growth factor-beta1 is a mediator of androgen-regulated growth arrest in an androgen-responsive prostatic cancer cell line, LNCaP. Endocrinology 1996, 137: 991-999. PMID: 8603613, DOI: 10.1210/endo.137.3.8603613.Peer-Reviewed Original ResearchConceptsDoses of dihydrotestosteroneProstatic cancer cell linesLNCaP cellsCancer cell linesTGF-beta1 messenger RNART-PCRCompetitive quantitative RT-PCRTGF-beta1 proteinDose-dependent increaseGrowth arrestEnzyme-linked immunoadsorbent assayCell linesTGF-beta1 neutralizing antibodyActivation of latentDose-response curveMessenger RNALNCaP proliferationQuantitative RT-PCRWestern blot analysisNeutralizing antibodiesLinear dose-response curveHigh doseTGF-beta1Immunoadsorbent assayGrowth factorGenetic change in transforming growth factor beta (TGF-beta) receptor type I gene correlates with insensitivity to TGF-beta 1 in human prostate cancer cells.
Kim I, Ahn H, Zelner D, Shaw J, Sensibar J, Kim J, Kato M, Lee C. Genetic change in transforming growth factor beta (TGF-beta) receptor type I gene correlates with insensitivity to TGF-beta 1 in human prostate cancer cells. Cancer Research 1996, 56: 44-8. PMID: 8548772.Peer-Reviewed Original ResearchConceptsProstate cancer cell linesLNCaP cellsProstate cancer cellsType I receptorT beta RCancer cell linesI geneDU145 cellsGenetic changesTGF-beta receptor type III receptorTGF-beta receptor expressionGrowth factor beta 1Beta RCancer cellsHuman prostate cancer cellsProliferation of PC3TGF-beta signalsBlot analysisReceptor type IICell linesDose-dependent mannerSouthern blot analysisType I geneType II receptor
1995
Regulation of proliferation and production of prostate-specific antigen in androgen-sensitive prostatic cancer cells, LNCaP, by dihydrotestosterone
Lee C, Sutkowski D, Sensibar J, Zelner D, Kim I, Amsel I, Shaw N, Prins G, Kozlowski J. Regulation of proliferation and production of prostate-specific antigen in androgen-sensitive prostatic cancer cells, LNCaP, by dihydrotestosterone. Endocrinology 1995, 136: 796-803. PMID: 7530653, DOI: 10.1210/endo.136.2.7530653.Peer-Reviewed Original ResearchConceptsHigher DHT concentrationsEffects of androgensConcentrations of dihydrotestosteroneDHT concentrationsPSA secretionAndrogen receptorCharcoal-stripped fetal bovine serumProstate-specific antigen (PSA) productionHuman prostatic cancer cell linesLow DHT concentrationsProstatic cancer cell linesDose-related mannerNuclear androgen receptorProstate-specific antigenCellular proliferationProstatic cancer cellsProduction of PSADose-dependent inductionWestern blot analysisCancer cell linesProportion of cellsDHT levelsLNCaP cellsM dihydrotestosteronePositive stainingRegulation of proliferation and production of prostate-specific antigen in androgen-sensitive prostatic cancer cells, LNCaP, by dihydrotestosterone
Lee C, Sutkowski D, Sensibar J, Zelner D, Kim I, Amsel I, Shaw N, Prins G, Kozlowski J. Regulation of proliferation and production of prostate-specific antigen in androgen-sensitive prostatic cancer cells, LNCaP, by dihydrotestosterone. Endocrinology 1995, 136: 796-803. DOI: 10.1210/en.136.2.796.Peer-Reviewed Original ResearchProstate-specific antigenProduction of prostate-specific antigenProstate-specific antigen secretionConcentrations of dihydrotestosteroneEffects of androgensDihydrotestosterone concentrationsAndrogen receptorAndrogen-sensitive human prostate cancer cell lineAndrogen-sensitive prostate cancer cellsIncreasing concentrations of DHTLow concentrations of dihydrotestosteroneCharcoal-stripped fetal bovine serumAnalysis of androgen receptorHuman prostate cancer cell linesProstate cancer cell linesCellular proliferationProstate cancer cellsNuclear androgen receptorAmount of receptor proteinDose-dependent inductionProportion of cellsFetal bovine serumCancer cell linesLNCaP cellsRegulation of proliferation