2025
Autoimmune mechanisms elucidated through muscle acetylcholine receptor structures
Li H, Pham M, Teng J, O'Connor K, Noviello C, Hibbs R. Autoimmune mechanisms elucidated through muscle acetylcholine receptor structures. Cell 2025, 188: 2390-2406.e20. PMID: 40203823, PMCID: PMC12118449, DOI: 10.1016/j.cell.2025.03.004.Peer-Reviewed Original ResearchConceptsMyasthenia gravisPatient-derived monoclonal antibodiesAntibody-mediated autoimmune disordersVariable patient responseDiverse pathogenic mechanismsAcetylcholine (AChMG immunopathogenesisHuman muscle AChRReceptor blockadeReceptor inhibitionAdult AChRAutoimmune mechanismsAutoimmune disordersChannel activitySkeletal muscle contractionMuscle weaknessEpitope diversityPathogenic mechanismsMuscle AChRIonotropic receptorsMonoclonal antibodiesComplement activationPatient responseMuscle contractionAChR
2023
YIV-818-A: a novel therapeutic agent in prostate cancer management through androgen receptor downregulation, glucocorticoid receptor inhibition, epigenetic regulation, and enhancement of apalutamide, darolutamide, and enzalutamide efficacy
Lam W, Arammash M, Cai W, Guan F, Jiang Z, Liu S, Cheng P, Cheng Y. YIV-818-A: a novel therapeutic agent in prostate cancer management through androgen receptor downregulation, glucocorticoid receptor inhibition, epigenetic regulation, and enhancement of apalutamide, darolutamide, and enzalutamide efficacy. Frontiers In Pharmacology 2023, 14: 1244655. PMID: 37860121, PMCID: PMC10582333, DOI: 10.3389/fphar.2023.1244655.Peer-Reviewed Original ResearchCastration-resistant prostate cancerAR target genesActive compoundsAnti-prostate cancer drugProstate cancerSynergistic effectGlucocorticoid receptorPotential drug candidatesDrug discovery platformRA-VIILuciferase activityKey active compoundsGlucocorticoid receptor inhibitionProstate cancer managementNovel therapeutic agentsRA-VDrug candidatesCompoundsDeprivation therapySafety profileCancer deathExtra-terminal (BET) proteinsGR activityReceptor inhibitionAR inhibition
2022
Epidermal Growth Factor Receptor Inhibition Is Protective in Hyperoxia‐Induced Lung Injury
Harris ZM, Sun Y, Joerns J, Clark B, Hu B, Korde A, Sharma L, Shin HJ, Manning EP, Placek L, Unutmaz D, Stanley G, Chun H, Sauler M, Rajagopalan G, Zhang X, Kang MJ, Koff JL. Epidermal Growth Factor Receptor Inhibition Is Protective in Hyperoxia‐Induced Lung Injury. Oxidative Medicine And Cellular Longevity 2022, 2022: 9518592. PMID: 36193076, PMCID: PMC9526641, DOI: 10.1155/2022/9518592.Peer-Reviewed Original ResearchConceptsAcute lung injuryEpidermal growth factor receptorAlveolar epithelial cellsLung injurySevere hyperoxiaEGFR inhibitionEpithelial cellsHyperoxia-Induced Lung InjuryRole of EGFRMurine alveolar epithelial cellsGrowth factor receptor inhibitionWorse clinical outcomesEpidermal growth factor receptor inhibitionHuman alveolar epithelial cellsWild-type littermatesPoly (ADP-ribose) polymeraseTerminal dUTP nickGrowth factor receptorClinical outcomesImproved survivalReceptor inhibitionLung repairProtective roleComplex roleEGFR deletion
2018
Obesity promotes resistance to anti-VEGF therapy in breast cancer by up-regulating IL-6 and potentially FGF-2
Incio J, Ligibel JA, McManus DT, Suboj P, Jung K, Kawaguchi K, Pinter M, Babykutty S, Chin SM, Vardam TD, Huang Y, Rahbari NN, Roberge S, Wang D, Gomes-Santos IL, Puchner SB, Schlett CL, Hoffmman U, Ancukiewicz M, Tolaney SM, Krop IE, Duda DG, Boucher Y, Fukumura D, Jain RK. Obesity promotes resistance to anti-VEGF therapy in breast cancer by up-regulating IL-6 and potentially FGF-2. Science Translational Medicine 2018, 10 PMID: 29540614, PMCID: PMC5936748, DOI: 10.1126/scitranslmed.aag0945.Peer-Reviewed Original ResearchConceptsVEGF therapyInterleukin-6Breast cancerMouse modelAnti-vascular endothelial growth factor therapyEndothelial growth factor therapyTumor vasculatureAnti-VEGF therapyAnti-VEGF treatmentIL-6 blockadeGrowth factor therapyIL-6 productionFGF-2Up-regulates IL-6Second mouse modelFGF-2 expressionTumor cell proliferationFactor therapyGrowth factor 2Proinflammatory factorsMetastatic sitesBC patientsObese miceReceptor inhibitionSystemic concentrations
2017
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N‑Methyl‑d‑aspartate (NMDA) Receptor Antagonist
Gynther M, Silvestri I, Hansen J, Hansen K, Malm T, Ishchenko Y, Larsen Y, Han L, Kayser S, Auriola S, Petsalo A, Nielsen B, Pickering D, Bunch L. Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N‑Methyl‑d‑aspartate (NMDA) Receptor Antagonist. Journal Of Medicinal Chemistry 2017, 60: 9885-9904. PMID: 29205034, PMCID: PMC5788303, DOI: 10.1021/acs.jmedchem.7b01624.Peer-Reviewed Original ResearchConceptsMurine hepatocellular carcinoma cellsHepatocellular carcinoma cellsN-methyl-D-aspartate receptor antagonistCompetitive N-methyl-D-aspartate (NMDA) receptor antagonistMultidrug resistanceCarcinoma cellsCancer cellsCommon solid tumorsNMDA receptor inhibitionIntrinsic multidrug resistanceReceptor antagonistReceptor inhibitionAnticancer drug efficacyUnderlying biological mechanismsSolid tumorsDrug efficacyReduced expressionCytotoxic actionSorafenibStructure-activity studiesMDR transportersAnticancer drugsBiological mechanismsCellsPromising strategyErbB activation signatures as potential biomarkers for anti-ErbB3 treatment in HNSCC
Alvarado D, Ligon GF, Lillquist JS, Seibel SB, Wallweber G, Neumeister VM, Rimm DL, McMahon G, LaVallee TM. ErbB activation signatures as potential biomarkers for anti-ErbB3 treatment in HNSCC. PLOS ONE 2017, 12: e0181356. PMID: 28723928, PMCID: PMC5517012, DOI: 10.1371/journal.pone.0181356.Peer-Reviewed Original ResearchConceptsNeuregulin-1NRG1 expressionErbB3 activationNeck squamous cell carcinomaSquamous cell carcinomaEnhanced anti-tumor activitySubset of HNSCCUnmet medical needHNSCC cell linesHNSCC patient samplesAnti-tumor activityGrowth factor αLigand neuregulin-1Cell carcinomaEGFR/ErbB familyHNSCC modelsCetuximab treatmentErbB receptor inhibitionReceptor inhibitionReceptor levelsRespective signaling pathwaysSolid tumorsTumor typesHNSCCPotential biomarkers
2015
Differential Effects of an NR2B NAM and Ketamine on Synaptic Potentiation and Gamma Synchrony: Relevance to Rapid-Onset Antidepressant Efficacy
Nagy D, Stoiljkovic M, Menniti FS, Hajós M. Differential Effects of an NR2B NAM and Ketamine on Synaptic Potentiation and Gamma Synchrony: Relevance to Rapid-Onset Antidepressant Efficacy. Neuropsychopharmacology 2015, 41: 1486-1494. PMID: 26404843, PMCID: PMC4832008, DOI: 10.1038/npp.2015.298.Peer-Reviewed Original ResearchConceptsAuditory-evoked potentialsAntidepressant effectsSynaptic potentiationAntidepressant efficacyAuditory gatingRapid-onset antidepressant effectsEffects of ketaminePrimary auditory cortexReceptor channel blockerDifferent acute effectsNMDA receptor inhibitionNegative allosteric modulatorsPotential mechanistic underpinningsReceptor inhibitionSystemic administrationAcute effectsNeurophysiological biomarkersTranslatable biomarkersChannel blockersDrug eliminationAuditory cortexNeurophysiological parametersDrug AdministrationGamma band powerKetamine
2013
Androgens influence microvascular dilation in PCOS through ET-A and ET-B receptors
Wenner MM, Taylor HS, Stachenfeld NS. Androgens influence microvascular dilation in PCOS through ET-A and ET-B receptors. AJP Endocrinology And Metabolism 2013, 305: e818-e825. PMID: 23921139, PMCID: PMC3798701, DOI: 10.1152/ajpendo.00343.2013.Peer-Reviewed Original ResearchConceptsPolycystic ovary syndromeET-B receptorsMicrovascular dilationHeat-induced vasodilationReceptor inhibitionET-B receptor antagonistGonadotropin-releasing hormone antagonistLaser Doppler flowmetryAndrogen suppressionOvary syndromeVascular dysfunctionHealthy womenT administrationEnhanced vasodilationHormone antagonistReceptor antagonistCutaneous microdialysisDoppler flowmetryTestosterone effectsSubtype receptorsVasodilationDay 8WomenDilationGnRHant
2010
Molecular Analysis of Non–Small Cell Lung Cancer Identifies Subsets with Different Sensitivity to Insulin-like Growth Factor I Receptor Inhibition
Gualberto A, Dolled-Filhart M, Gustavson M, Christiansen J, Wang YF, Hixon ML, Reynolds J, McDonald S, Ang A, Rimm DL, Langer CJ, Blakely J, Garland L, Paz-Ares LG, Karp DD, Lee AV. Molecular Analysis of Non–Small Cell Lung Cancer Identifies Subsets with Different Sensitivity to Insulin-like Growth Factor I Receptor Inhibition. Clinical Cancer Research 2010, 16: 4654-4665. PMID: 20670944, PMCID: PMC2952544, DOI: 10.1158/1078-0432.ccr-10-0089.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAntibodies, MonoclonalAntineoplastic AgentsCarcinoma, Non-Small-Cell LungClinical Trials, Phase II as TopicDrug Resistance, NeoplasmFemaleHormone AntagonistsHumansImmunoglobulins, IntravenousInsulin-Like Growth Factor IMaleMiceMolecular Diagnostic TechniquesNIH 3T3 CellsPrognosisRetrospective StudiesTissue Array AnalysisConceptsNon-small cell lung cancerPhase II studySquamous cell tumorsIGF-IRII studyCell tumorsStage IIIB/IV non-small cell lung cancerAdvanced non-small cell lung cancerCell lung cancerIGF-IR pathwayIGF-IR inhibitionIGF-IR expressionCombination of chemotherapyHigh response rateEpidermal growth factor receptorEpithelial-like tumorsInsulin receptor substrate-1Growth factor receptorHistologic subtypeTransitional tumorsReceptor therapyIGF-IILung cancerReceptor inhibitionIGF-IIR
2006
Epidermal Growth Factor Receptor Inhibitors in Development for the Treatment of Non–Small Cell Lung Cancer
Heymach JV, Nilsson M, Blumenschein G, Papadimitrakopoulou V, Herbst R. Epidermal Growth Factor Receptor Inhibitors in Development for the Treatment of Non–Small Cell Lung Cancer. Clinical Cancer Research 2006, 12: 4441s-4445s. PMID: 16857825, DOI: 10.1158/1078-0432.ccr-06-0286.Peer-Reviewed Original ResearchConceptsNon-small cell lung cancerCell lung cancerExtensive clinical testingLung cancerClinical testingRandomized phase II clinical trialEpidermal growth factor receptor inhibitor erlotinibPhase III clinical testingEpidermal growth factor receptor inhibitorsPhase II clinical trialGrowth factor receptor inhibitorsVascular endothelial growth factor receptorEndothelial growth factor receptorAdvanced clinical testingMultiple EGFR family membersGrowth factor receptorReceptor inhibitionClinical trialsEGFR family membersClinical activityReceptor inhibitorsPreclinical studiesInhibitor erlotinibClinical developmentSolid tumors
2003
Paradigm shift in neuroprotective drug development: clinically tolerated NMDA receptor inhibition by memantine
Lipton S, Chen H. Paradigm shift in neuroprotective drug development: clinically tolerated NMDA receptor inhibition by memantine. Cell Death & Differentiation 2003, 11: 18-20. PMID: 14647237, DOI: 10.1038/sj.cdd.4401344.Peer-Reviewed Original ResearchAdjunctive platelet glycoprotein IIb/IIIa receptor inhibition with tirofiban before primary angioplasty improves angiographic outcomes: results of the tirofiban given in the emergency room before primary angioplasty (TIGER-PA) pilot trial
Lee D, Herity N, Hiatt B, Trial T. Adjunctive platelet glycoprotein IIb/IIIa receptor inhibition with tirofiban before primary angioplasty improves angiographic outcomes: results of the tirofiban given in the emergency room before primary angioplasty (TIGER-PA) pilot trial. ACC Current Journal Review 2003, 12: 67. DOI: 10.1016/s1062-1458(03)00308-8.Peer-Reviewed Original Research
2002
Neuroprotective role of δ-opioid receptors in cortical neurons
Zhang J, Gibney GT, Zhao P, Xia Y. Neuroprotective role of δ-opioid receptors in cortical neurons. American Journal Of Physiology - Cell Physiology 2002, 282: c1225-c1234. PMID: 11997236, DOI: 10.1152/ajpcell.00226.2001.Peer-Reviewed Original ResearchConceptsCortical neuronsNeuronal injuryHypoxic injuryReceptor activationKappa-opioid receptor inhibitionDelta-opioid receptor activationOpioid receptor activationCultured cortical neuronsGlutamate-induced injuryΔ-opioid receptorsLactate dehydrogenase releaseImmature neuronsNeuroprotective roleReceptor inhibitionHypoxic exposureNeuronal susceptibilityCell injuryDay 4InjuryDehydrogenase releaseNeuronsActivation/inhibitionHypoxiaHypoxic conditionsHypoxic stressPharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition.
Albanell J, Rojo F, Averbuch S, Feyereislova A, Mascaro J, Herbst R, LoRusso P, Rischin D, Sauleda S, Gee J, Nicholson R, Baselga J. Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition. Journal Of Clinical Oncology 2002, 20: 110-24. PMID: 11773160, DOI: 10.1200/jco.2002.20.1.110.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralAdultAgedAntineoplastic AgentsApoptosisBiomarkersCell Cycle ProteinsCyclin-Dependent Kinase Inhibitor p27Dose-Response Relationship, DrugErbB ReceptorsFemaleGefitinibHumansKeratinocytesMaleMAP Kinase Signaling SystemMiddle AgedNeoplasmsQuinazolinesSkinStatistics, NonparametricTumor Suppressor ProteinsConceptsCancer patientsEpidermal growth factor receptor tyrosine kinase inhibitor ZD1839Tyrosine kinase inhibitor ZD1839Phase I clinical trialMaximum-tolerated doseDose-limiting toxicityEGFR activationReceptor-dependent processUnacceptable toxicityDefinitive efficacyPharmacodynamic assessmentSafety trialPharmacodynamic effectsClinical trialsKeratin plugsReceptor inhibitionMaturation markersSkin biopsiesPharmacodynamic studiesProliferation indexDose levelsOral ZD1839PatientsOptimal dosesZD1839
2001
Pharmacodynamic studies of the specific oral EGFR tyrosine kinase inhibitor (EGFR-TKI) zd1839 (‘Iressa’) in skin from cancer patients participating in phase I trials: histopathological and molecular consequences of receptor inhibition
Albanell J, Rojo F, Averbuch S, Feyereislova A, Herbst R, LoRusso P, Rischin D, Gee J, Nicholson R, Baselga J. Pharmacodynamic studies of the specific oral EGFR tyrosine kinase inhibitor (EGFR-TKI) zd1839 (‘Iressa’) in skin from cancer patients participating in phase I trials: histopathological and molecular consequences of receptor inhibition. European Journal Of Cancer 2001, 37: s159. DOI: 10.1016/s0959-8049(01)81071-6.Peer-Reviewed Original Research
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