Search results for "Assays"

showing 10 items of 546 documents

Retinol oxidation to retinoic acid in human thyroid glandular cells.

2014

Abstract Retinoic acid is regarded as the retinol metabolite that controls proliferation and differentiation of epithelial cells. In the present study, we investigated the potential role of xanthine dehydrogenase (XDH) in retinoic acid biosynthesis in human thyroid glandular cells (HTGC). In particular, we observed that cellular retinoids binding proteins (CRBPs) are also implicated in the biosynthetic pathway leading to retinoic acid formation in primary cultures of HTGC, as we have already reported for human mammary epithelial cells (HMEC). After partial protein purification, the enzyme responsible for retinoic acid biosynthesis was identified and quantified as XDH by immunoassay, by its …

AdultMaleXanthine DehydrogenasePrimary Cell CultureRetinoic acidThyroid GlandOxypurinolRetinoic acid receptor betaTretinoinBiologyXanthinechemistry.chemical_compoundBiosynthesisSettore BIO/10 - BiochimicaDrug DiscoveryHumansEnzyme InhibitorsVitamin AEnzyme AssaysPharmacologyImmunoassayRetinolEpithelial CellsRetinol-Binding Proteins CellularGeneral MedicineMiddle AgedXanthineUric AcidRetinoic acid receptorchemistryXanthine dehydrogenaseBiochemistryCRABPs CRBPs human glandular cells. retinoic acid biosynthesis. retinol oxidation xanthine dehydrogenaseUric acidFemaleOxidation-ReductionJournal of enzyme inhibition and medicinal chemistry
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Relationship Between Glucocerebrosidase Activity and Clinical Response to Enzyme Replacement Therapy in Patients With Gaucher Disease Type I

2018

The quantification of enzyme activity in the patient treated with enzyme replacement therapy (ERT) has been suggested as a tool for dosage individualization, so we conducted a study to evaluate the relationship between glucocerebrosidase activity and clinical response in patients with Gaucher disease type I (GD1) to ERT. The study included patients diagnosed with GD1, who were being treated with ERT, and healthy individuals. Markers based on glucocerebrosidase activity measurement in patients' leucocytes were studied: enzyme activity at 15 min. post-infusion (Act75 ) reflects the amount of enzyme that is distributed in the body post-ERT infusion, and accumulated glucocerebrosidase activity …

AdultMalecongenital hereditary and neonatal diseases and abnormalitiesmedicine.medical_specialtyDiseaseToxicologySeverity of Illness IndexGastroenterology03 medical and health sciencesGlucocerebrosidase activity0302 clinical medicineStatistical significanceInternal medicineLeukocytesHumansMedicineEnzyme Replacement TherapyIn patientProspective Studies030212 general & internal medicineInverse correlationAgedEnzyme AssaysPharmacologyGaucher DiseaseDose-Response Relationship Drugbiologybusiness.industryArea under the curvenutritional and metabolic diseasesGeneral MedicineEnzyme replacement therapyMiddle AgedEnzyme assayTreatment Outcome030220 oncology & carcinogenesisbiology.proteinGlucosylceramidaseFemalebusinessBiomarkersFollow-Up StudiesBasic & Clinical Pharmacology & Toxicology
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Blockade of nicotinic and muscarinic receptors facilitates spontaneous migration of human peripheral granulocytes: failure in cystic fibrosis.

2012

Circulating leucocytes express muscarinic (m) and nicotinic (n) receptors and synthesize acetylcholine (ACh) regulating various cell functions. Leucocytes from patients with cystic fibrosis contain less ACh; therefore it was tested whether the regulation of cellular functions like migration differed from healthy volunteers.Peripheral blood (10-20 ml) was used, leucocytes were isolated by Ficoll® gradient and the commercial MIGRATEST® combined with flow cytometric analysis was applied (pore size 3 μm).In the absence of test substances 4900±1800 (n=10) leucocytes migrated within a time period of 2 h. In the presence of tubocurarine (TC, 30 μM) the cell number increased to 7500±2700 [n=10] cor…

AdultMalemedicine.medical_specialtyAdolescentCystic FibrosisBiologyReceptors NicotinicGeneral Biochemistry Genetics and Molecular BiologyCholinergic AntagonistsYoung AdultCell Migration Assays LeukocyteCell MovementInternal medicineMuscarinic acetylcholine receptormedicineMuscarinic acetylcholine receptor M4HumansGeneral Pharmacology Toxicology and PharmaceuticsReceptorChildMuscarinic acetylcholine receptor M3Muscarinic acetylcholine receptor M2General MedicineReceptors MuscarinicNicotinic agonistEndocrinologyCholinergicFemaleAcetylcholinemedicine.drugGranulocytesLife sciences
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Comparison of anti-transglutaminase ELISAs and an anti-endomysial antibody assay in the diagnosis of celiac disease: A prospective study

2002

Abstract Background: Most studies of anti-transglutaminase (anti-tTG) assays have considered preselected groups of patients. This study compared the sensitivity, specificity, and predictive value of an immunofluorescence method for anti-endomysial antibodies (EmAs) and two anti-tTG ELISAs, one using guinea pig tTG (gp-tTG) and the other human tTG (h-tTG) as antigen, in consecutive patients investigated for suspected celiac disease (CD). Methods: We studied 207 consecutive patients (99 men, 108 women; age range, 17–84 years) who underwent intestinal biopsy for suspected CD. Patients presented with one or more of the following: weight loss, anemia, chronic diarrhea, abdominal pain, dyspepsia,…

AdultMalemedicine.medical_specialtyPathologyanti-endomysial antibodieSettore MED/09 - Medicina InternaAdolescentTissue transglutaminaseAnemiaClinical BiochemistryGuinea PigsEnzyme-Linked Immunosorbent AssayChronic liver diseaseGastroenterologyCoeliac diseaseEsophagusAntibody SpecificityPredictive Value of TestsInternal medicineImmunopathologymedicineAnimalsHumansanti-transglutaminase; assays; anti-endomysial antibodies; celiac diseaseProspective StudiesProspective cohort studyAgedAutoantibodiesAged 80 and overTransglutaminasesbiologybusiness.industryBiochemistry (medical)HaplorhiniassayMiddle Agedmedicine.diseaseEndomysiumImmunoglobulin ACeliac Diseasemedicine.anatomical_structurePredictive value of testsbiology.proteinFemaleanti-transglutaminasebusiness
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Evaluation of the antiproliferative, proapoptotic, and antiangiogenic effects of a double-stranded RNA mimic complexed with polycations in an experim…

2015

Objective To assess the antiproliferative, proapoptotic, and antiangiogenic effects of the double-stranded RNA mimic polyinosine-polycytidylic acid (pIC) complexed with polyethylenimine [pIC PEI ] in xenografted human leiomyomas. Design Heterologous leiomyoma mouse model. Setting University-affiliated infertility center. Animal(s) Ovariectomized and hormone-replaced nude mice (n = 16) who received human leiomyoma fragment transplantation. Intervention(s) Leiomyoma fragments placed in the peritoneum of 5-week-old nude female mice and treated with the vehicle (n = 8) or 0.6 mg/kg [pIC PEI ] (n = 8) for 4 weeks. Main Outcome Measure(s) The size of the leiomyoma implants, and cellular prolifera…

AdultTime FactorsAngiogenesisOvariectomyHeterologousMice NudeAngiogenesis InhibitorsApoptosis03 medical and health scienceschemistry.chemical_compound0302 clinical medicinePeritoneummedicineTumor Cells CulturedAnimalsHumansPolyethyleneimineCell ProliferationPolyethylenimine030219 obstetrics & reproductive medicineLeiomyomaNeovascularization PathologicCell growthbusiness.industryEstrogen Replacement TherapyObstetrics and GynecologyMiddle Agedmedicine.diseaseXenograft Model Antitumor AssaysTumor BurdenTransplantationPlatelet Endothelial Cell Adhesion Molecule-1Disease Models AnimalLeiomyomamedicine.anatomical_structureKi-67 AntigenPoly I-CReproductive MedicinechemistryApoptosis030220 oncology & carcinogenesisImmunologyUterine NeoplasmsCancer researchFemalebusinessFertility and sterility
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Improving ovarian tissue cryopreservation for oncologic patients: slow freezing versus vitrification, effect of different procedures and devices.

2013

Objective To compare slow freezing (SF) with four vitrification techniques (VT) for cryopreservation of ovarian tissue (OT) and to evaluate the best protocol for human OT in a xenograft model. Design Experimental study. Setting University hospital. Patient(s) Patients undergoing fertility preservation. Animal(s) Ovariectomized nude mice. Intervention(s) Cryopreservation of bovine OT after SF and four VTs (VT1, VT2, VT3, and VT4) by combining two cryoprotectant vitrification solutions (VS1 and VS2) and two devices (metallic grid and ethyl vinyl acetate bag), after which the cryopreservation of human OT by SF and VT1 and xenograft into nude mice. Main Outcome Measure(s) Follicular densities, …

AdultTime FactorsCryoprotectantAdolescentPopulationMice NudeBreast NeoplasmsBiologyCryopreservationAndrologyMiceRandom AllocationYoung AdultFresh TissueFollicular phaseAnimalsHumansVitrificationOvarian tissue cryopreservationeducationCell ProliferationCryopreservationeducation.field_of_studyOvaryObstetrics and GynecologyFertility PreservationHodgkin DiseaseVitrificationXenograft Model Antitumor AssaysTransplantationTreatment OutcomeReproductive MedicineImmunologyCattleFemaleFertility and sterility
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Nociceptin/orphanin FQ opioid receptor (NOP) selective ligand MCOPPB links anxiolytic and senolytic effects

2021

Accumulation of senescent cells may drive age-associated alterations and pathologies. Senolytics are promising therapeutics that can preferentially eliminate senescent cells. Here, we performed a high-throughput automatized screening (HTS) of the commercial LOPAC®Pfizer library on aphidicolin-induced senescent human fibroblasts, to identify novel senolytics. We discovered the nociceptin receptor FQ opioid receptor (NOP) selective ligand 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole (MCOPPB, a compound previously studied as potential anxiolytic) as the best scoring hit. The ability of MCOPPB to eliminate senescent cells in in vitro models was further tested…

Agingmedicine.drug_classNarcotic AntagonistsNOPMCOPPBSenescenceLigandsAnxiolyticMice03 medical and health scienceschemistry.chemical_compound0302 clinical medicinePiperidinesSenotherapeuticsOpioid receptormedicineAnimalsHumansSenolyticCaenorhabditis elegansReceptorSenolyticCellular Senescence030304 developmental biology0303 health sciencesNOPSenolytic.ChemistryLigand (biochemistry)High-Throughput Screening Assays3. Good healthCell biologyAnalgesics OpioidNociceptin receptorAnti-Anxiety AgentsOpioid PeptidesReceptors OpioidOriginal ArticleGeriatrics and Gerontology030217 neurology & neurosurgeryGeroScience
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Irreversible Inhibition of Epidermal Growth Factor Receptor Activity by 3-Aminopropanamides

2012

Irreversible epidermal growth factor receptor (EGFR) inhibitors contain a reactive warhead which covalently interacts with a conserved cysteine residue in the kinase domain. The acrylamide fragment, a commonly employed warhead, effectively alkylates Cys797 of EGFR, but its reactivity can cause rapid metabolic deactivation or nonspecific reactions with off-targets. We describe here a new series of irreversible inhibitors containing a 3-aminopropanamide linked in position 6 to 4-anilinoquinazoline or 4-anilinoquinoline-3- carbonitrile driving portions. Some of these compounds proved to be as efficient as their acrylamide analogues in inhibiting EGFR-TK (TK = tyrosine kinase) autophosphorylati…

AmideCell SurvivalEGFR inhibitorsQuinolineAntineoplastic AgentsAntineoplastic AgentStructure-Activity RelationshipT790MGefitinibCell Line TumorDrug DiscoveryPropionatemedicineHumansStructure–activity relationshipEpidermal growth factor receptorPhosphorylationAniline CompoundsbiologyChemistryDrug Discovery3003 Pharmaceutical ScienceAutophosphorylationQuinazolineAniline CompoundAmidesSettore CHIM/08 - Chimica FarmaceuticaErbB ReceptorsBiochemistryProtein kinase domainDrug Resistance NeoplasmQuinazolinesQuinolinesbiology.proteinMolecular MedicinePhosphorylationReceptor Epidermal Growth FactorPropionatesDrug Screening Assays AntitumorTyrosine kinaseHumanmedicine.drugJournal of Medicinal Chemistry
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Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening

2013

The design through energy-based pharmacophore virtual screening has led to aminocyanopyridine derivatives as efficacious new inhibitors of Hsp90. The synthesized compounds showed a good affinity for the Hsp90 ATP binding site in the competitive binding assay. Moreover, they showed an excellent antiproliferative activity against a large number of human tumor cell lines. Further biological studies on the derivative with the higher EC50 confirmed its specific influence on the cellular pathways involving Hsp90.

AminopyridinesInhibitory Concentration 50Structure-Activity RelationshipUser-Computer InterfaceHeat shock proteinCell Line TumorSettore BIO/10 - BiochimicaDrug DiscoveryHumansHSP90 Heat-Shock ProteinsBinding siteVirtual screeningheat shock protein 90 inhibitors energy-based pharmacophore virtual screening cell cycle antiproliferative activitybiologyChemistryHsp90Combinatorial chemistrySettore CHIM/08 - Chimica FarmaceuticaHuman tumorMolecular Docking SimulationCell cultureDrug DesignEnergy basedbiology.proteinMolecular MedicinePharmacophoreDrug Screening Assays Antitumor
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Apoptotic effects of different drugs on cultured retinoblastoma Y79 cells

1998

This paper deals with the apoptotic effect exerted in human retinoblastoma Y79 cells by a number of compounds. A remarkable effect was observed after treatment with DNA-damaging agents, such as camptothecin, etoposide, cisplatin and carboplatin; camptothecin was found to be the most efficacious. Treatment with these compounds induced the appearance of morphological features of apoptosis in the cells together with the distinct fragmentation of DNA, as shown by agarose gel electrophoresis. These effects were also accompanied by a remarkable increase in the level of p53. Many other compounds, which are not DNA-damaging agents, induced the morphological features of apoptosis but none of them we…

AmsacrinePaclitaxelDNA damageAntineoplastic AgentsApoptosisSuraminDNA ladderingBiologyretinoblastomaCarboplatinchemistry.chemical_compoundTumor Cells CulturedmedicineHumansFragmentation (cell biology)EtoposideCisplatinSodium butyrateGeneral MedicineAntineoplastic Agents PhytogenicMolecular biologyButyrateschemistryApoptosisAgarose gel electrophoresisImmunologyButyric AcidCamptothecinCisplatinDrug Screening Assays AntitumorCamptothecinDNA Damagemedicine.drug
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