Search results for "Transporter"

showing 10 items of 676 documents

Cytotoxicity of the indole alkaloid reserpine from Rauwolfia serpentina against drug-resistant tumor cells.

2015

Abstract Background: The antihypertensive reserpine is an indole alkaloid from Rauwolfia serpentina and exerts also profound activity against cancer cells in vitro and in vivo. The present investigation was undertaken to investigate possible modes of action to explain its activity toward drug-resistant tumor cells. Material and methods: Sensitive and drug-resistant tumor cell lines overexpressing P-glycoprotein (ABCB1/MDR1), breast cancer resistance protein (ABCG2/BCRP), mutation-activated epidermal growth factor receptor (EGFR), wild-type and p53-knockout cells as well as the NCI panel of cell lines from different tumor origin were analyzed. Reserpine's cytotoxicity was investigated by res…

ATP Binding Cassette Transporter Subfamily BReserpineAngiogenesisPharmaceutical SciencePharmacologyBiologyRauwolfiaGene Knockout TechniquesCell Line TumorDrug DiscoverymedicineATP Binding Cassette Transporter Subfamily G Member 2HumansCytotoxicityPharmacologyWnt signaling pathwayReserpineAntineoplastic Agents PhytogenicDrug Resistance MultipleNeoplasm ProteinsErbB ReceptorsMolecular Docking SimulationComplementary and alternative medicineCell cultureApoptosisDoxorubicinDrug Resistance NeoplasmCancer cellMolecular MedicineATP-Binding Cassette TransportersErlotinibTumor Suppressor Protein p53medicine.drugPhytomedicine : international journal of phytotherapy and phytopharmacology
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Selective downregulation of the MDR1 gene product in Caco-2 cells by stable transfection to prove its relevance in secretory drug transport.

2005

Considerable interest is focused on overcoming multidrug resistance (MDR) in cancer chemotherapy. The in vitro experiments to characterize P-glycoprotein's (P-gp) function and to decrease its effects have led to a variety of strategies such as addition of competitors or supplementation of the medium with oligonucleotides complementary to the 5'-end of the MDR1-mRNA. For the Caco-2 cell line, an in vitro model for absorption screening, expressing multiple transporters including P-gp, which pumps substances back into the apical solution, P-gp activity might mask other relevant transport proteins' activity. The objective of the present study was to construct a Caco-2 subline with reduced P-gp …

ATP Binding Cassette Transporter Subfamily BTime FactorsPharmaceutical ScienceDown-RegulationBiologyTransfectionPermeabilityPropanolaminesDownregulation and upregulationDrug DiscoveryHumansNorthern blotOligonucleotideReverse Transcriptase Polymerase Chain ReactionElectroporationBiological TransportTransfectionFlow CytometryMolecular biologyIn vitroTransport proteinClone CellsMutagenesis InsertionalVerapamilCell cultureMolecular MedicineCaco-2 CellsGenes MDRMolecular pharmaceutics
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Pharmacogenomic Characterization of Cytotoxic Compounds from Salvia officinalis in Cancer Cells.

2015

Salvia officinalis is used as a dietary supplement with diverse medicinal activity (e.g. antidiabetic and antiatherosclerotic effects). The plant also exerts profound cytotoxicity toward cancer cells. Here, we investigated possible modes of action to explain its activity toward drug-resistant tumor cells. Log10IC50 values of two constituents of S. officinalis (ursolic acid, pomolic acid) were correlated to the expression of ATP-binding cassette (ABC) transporters (P-glycoprotein/ABCB1/MDR1, MRP1/ABCC1, BCRP/ABCG2) and epidermal growth factor receptor (EGFR) or mutations in RAS oncogenes and the tumor suppressor gene TP53 of the NCI panel of cell lines. Gene expression profiles predicting se…

ATP Binding Cassette Transporter Subfamily BTumor suppressor geneLeupeptinsPharmaceutical ScienceATP-binding cassette transporterBreast NeoplasmsBiologymedicine.disease_causeAnalytical Chemistrychemistry.chemical_compoundfoodUrsolic acidDrug DiscoveryGene expressionmedicineHumansOleanolic AcidSalvia officinalisPharmacologyMutationPlants MedicinalMolecular StructureOrganic ChemistrySalvia officinalisNF-kappa BGenes erbB-1Antineoplastic Agents Phytogenicfood.foodTriterpenesComplementary and alternative medicinechemistryBiochemistryDrug Resistance NeoplasmPharmacogeneticsCancer cellMolecular MedicineATP-Binding Cassette TransportersSignal transductionSignal TransductionJournal of natural products
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Binding mode analysis of ABCA7 for the prediction of novel Alzheimer's disease therapeutics

2021

Graphical abstract

ATP Adenosine-triphosphateNBD nucleotide binding domainGSH reduced glutathionePolypharmacologyAlzheimer’s disease (AD)ATP-binding cassette transporterHTS high-throughput screeningBiochemistryABCA7Structural BiologyPLIF protein ligand interactionMSD membrane spanning domainPDB protein data bankTM transmembrane helixABC ATP-binding cassetteMultitarget modulation (PANABC)RMSD root mean square distanceABC transporter (ABCA1 ABCA4 ABCA7)Computer Science ApplicationsMOE Molecular Operating EnvironmentPharmacophoreSNP single-nucleotide polymorphismBiotechnologyResearch ArticleBBB blood-brain barrierBiophysicsDrug designComputational biologyBiologyAD Alzheimer’s diseasePET positron emission tomographyIC intracellular helixAPP amyloid precursor proteincryo-EM cryogenic-electron microscopyGeneticsHomology modelingBinding siteRational drug design and developmentComputingMethodologies_COMPUTERGRAPHICSNBD-cholesterol 7-nitro-2-13-benzoxadiazol-4-yl-cholesterolTransporterPSO particle swarm optimizationPET tracer (PETABC)ECD extracellular domainR-domain/region regulatory domain/regionABCA1biology.proteinEH extracellular helixTP248.13-248.65BODIPY-cholesterol 44-difluoro-4-bora-3a4a-diaza-s-indacene-cholesterolComputational and Structural Biotechnology Journal
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Inhibition of ATP-Binding Cassette Transporters by Chinese Herbs and Phytochemicals

2012

The gene family of ATP-binding cassette (ABC) transporters is widely distributed over the evolutionary tree of life from bacteria to man. In cancer, several ABC transporters are involved in the transport of anticancer drugs. This leads to the development of resistance to a broad spectrum of anticancer agents, termed multidrug resistance. An attractive strategy to overcome multidrug resistance is to block the transport function of ABC transporters leading to lethal intracellular concentrations of anticancer drugs. Efforts to identify transport inhibitors lead to a huge amount of chemical substances, none of which successfully passed clinical trials in cancer patients because of high toxicity…

Abcg2CancerATP-binding cassette transporterTransporterBiologymedicine.diseaseMultiple drug resistancechemistry.chemical_compoundchemistryBiochemistrymedicinebiology.proteinGene familyXenobioticFunction (biology)
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Cytotoxicity of cucurbitacin E from Citrullus colocynthis against multidrug-resistant cancer cells

2019

Abstract Background Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad. Purpose This study outlines CuE's cytotoxic activity against drug-resistant tumor cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR). Methods Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towar…

Abcg2Drug ResistancePharmaceutical ScienceATP-binding cassette transporterMicroarraySubfamily Gchemistry.chemical_compoundGene Knockout Techniques0302 clinical medicineEpidermal growth factorPhytogenicDrug DiscoveryATP Binding Cassette Transporter Subfamily G Member 2Cancer0303 health sciencesTumorLeukemiabiologyChemistryABCB5TransfectionCell cycleNeoplasm ProteinsGene Expression Regulation NeoplasticErbB ReceptorsMolecular Docking SimulationSubfamily B030220 oncology & carcinogenesisMolecular MedicineCitrullus colocynthiMember 2Member 1ATP Binding Cassette Transporter Subfamily BATP Binding Cassette TransporterAntineoplastic AgentsCell Line03 medical and health sciencesCell Line TumorHumansATP Binding Cassette Transporter Subfamily B Member 1030304 developmental biologyCucurbitacin EPharmacologyNeoplasticTraditional herbal medicineCancer; Citrullus colocynthis; Drug resistance; Microarray; Traditional herbal medicine; ATP Binding Cassette Transporter Subfamily B; ATP Binding Cassette Transporter Subfamily B Member 1; ATP Binding Cassette Transporter Subfamily G Member 2; Antineoplastic Agents Phytogenic; Cell Line Tumor; Citrullus colocynthis; Doxorubicin; Drug Resistance Neoplasm; ErbB Receptors; Gene Expression Regulation Neoplastic; Gene Knockout Techniques; Humans; Leukemia; Molecular Docking Simulation; Neoplasm Proteins; Triterpenes; Tumor Suppressor Protein p53Antineoplastic Agents PhytogenicTriterpenesComplementary and alternative medicineGene Expression RegulationDrug Resistance NeoplasmDoxorubicinCancer cellbiology.proteinCancer researchNeoplasmCitrullus colocynthisTumor Suppressor Protein p53
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Trans-epithelial transport of the betalain pigments indicaxanthin and betanin across Caco-2 cell monolayers and influence of food matrix.

2012

Purpose: This study investigated the absorption mechanism of the phytochemicals indicaxanthin and betanin and the influence of their food matrix (cactus pear and red beet) on the intestinal transport. Methods: Trans-epithelial transport of dietary-consistent amounts of indicaxanthin and betanin in Caco-2 cell monolayers seeded on TranswellR inserts was measured in apical to basolateral (AP-BL) and basolateral to apical (BL-AP) direction, under an inwardly directed pH gradient (pH 6.0/7.4, AP/BL) mimicking luminal and serosal sides of human intestinal epithelium. The effect of inhibitors of membrane transporters on the absorption was also evaluated. Contribution of the paracellular route was…

Absorption (pharmacology)Cell Membrane PermeabilityChemical PhenomenaPyridinesBetalainsindicaxanthinMedicine (miscellaneous)Plant RootsIntestinal absorptionAntioxidantsCaco-2 cellchemistry.chemical_compoundPigmentSettore BIO/10 - BiochimicaHumansbetalains;intestinal absorption; Caco-2 cells; betalainic food; indicaxanthin; betaninFood scienceIntestinal MucosaBetaninbetalainic foodPEARNutrition and DieteticsbetaninbetalainCell PolarityFood Coloring AgentsOpuntiaBiological TransportPigments BiologicalBetaxanthinsIntercellular JunctionschemistryIntestinal AbsorptionCaco-2visual_artFruitFood Fortifiedvisual_art.visual_art_mediumATP-Binding Cassette TransportersDigestionBetacyaninsBeta vulgarisCaco-2 CellsDigestionIndicaxanthinEuropean journal of nutrition
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A double-negative (IgD−CD27−) B cell population is increased in the peripheral blood of elderly people

2009

The T cell branch of the immune system has been extensively studied in the elderly and it is known that the elderly have impaired immune function, mainly due to the chronic antigenic load that ultimately causes shrinkage of the T cell repertoire and filling of the immunologic space with memory T cells. In the present paper, we describe the IgD(-)CD27(-) double-negative B cell population which (as we have recently described) is higher in the elderly. Most of these cells were IgG(+). Evaluation of the telomere length and expression of the ABCB1 transporter and anti-apoptotic molecule, Bcl2, shows that they have the markers of memory B cells. We also show that these cells do not act as antigen…

AdultAgingATP Binding Cassette Transporter Subfamily BT cellAntigens CD19B-Lymphocyte Subsetschemical and pharmacologic phenomenaYoung AdultB lymphocyte Immunosenescence IgD CD27 Elderly Immunologic memorymedicineHumansCytotoxic T cellATP Binding Cassette Transporter Subfamily B Member 1IL-2 receptorCD40 AntigensCD154Antigen-presenting cellCells CulturedAgedAged 80 and overSettore MED/04 - Patologia Generalebusiness.industryAge FactorsHLA-DR AntigensImmunoglobulin DMiddle AgedTelomereFlow CytometryAcquired immune systemTumor Necrosis Factor Receptor Superfamily Member 7B-1 cellKi-67 Antigenmedicine.anatomical_structureProto-Oncogene Proteins c-bcl-2ImmunologyB7-1 AntigenbusinessImmunologic MemoryCD80Developmental BiologyMechanisms of Ageing and Development
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Clinical profiles and quality of care of subjects with type 2 diabetes according to their cardiovascular risk: an observational, retrospective study

2021

Abstract Background The European Society of Cardiology (ESC) recently defined cardiovascular risk classes for subjects with diabetes. Aim of this study was to explore the distribution of subjects with type 2 diabetes (T2D) by cardiovascular risk groups according to the ESC classification and to describe the quality indicators of care, with particular regard to cardiovascular risk factors. Methods The study is based on data extracted from electronic medical records of patients treated at the 258 Italian diabetes centers participating in the AMD Annals initiative. Patients with T2D were stratified by cardiovascular risk. General descriptive indicators, measures of intermediate outcomes, inten…

AdultBlood GlucoseMalelcsh:Diseases of the circulatory (Cardiovascular) systemmedicine.medical_specialtyTime FactorsEndocrinology Diabetes and MetabolismType 2 diabetesIncretinsRisk AssessmentDiabetes mellitusInternal medicinemedicineElectronic Health RecordsHumansHypoglycemic AgentsMedical prescriptionSodium-Glucose Transporter 2 InhibitorsOriginal InvestigationAgedQuality Indicators Health CareRetrospective StudiesAngiologyCardiovascular risk Humans Hypoglycemic Agents Incretins Italy Male Middle Aged Retrospective Studies Risk Assessment Sodium-Glucose Transporter 2 Inhibitors Time Factors Treatment Outcome Quality Indicators Health Care Quality of care Type 2 diabetes Adult Aged Aged 80 and over Biomarkers Blood Glucose Cardiovascular Diseases Diabetes Mellitus Type 2 Dipeptidyl-Peptidase IV Inhibitors Heart Disease Risk Factors Female Electronic Health RecordsAged 80 and overDipeptidyl-Peptidase IV Inhibitorsbusiness.industryMedical recordQuality of careType 2 diabetesRetrospective cohort studyMiddle AgedCardiovascular riskmedicine.diseaseTreatment OutcomeDiabetes Mellitus Type 2ItalyCardiovascular DiseasesHeart Disease Risk Factorslcsh:RC666-701AlbuminuriaFemaleObservational studymedicine.symptomCardiology and Cardiovascular MedicinebusinessBiomarkersCardiovascular Diabetology
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Impact of combinations of single-nucleotide polymorphisms of anthracycline transporter genes upon the efficacy and toxicity of induction chemotherapy…

2020

Anthracycline uptake could be affected by influx and efflux transporters in acute myeloid leukemia (AML). Combinations of single-nucleotide polymorphisms (SNPs) of wild-type genotype of influx transporters (SLC22A16, SLCO1B1) and homozygous variant genotypes of ABC polymorphisms (ABCB1, ABCC1, ABCC2, ABCG2) were evaluated in 225 adult de novo AML patients. No differences in complete remission were reported, but higher induction death was observed with combinations of SLCO1B1 rs4149056 and ABCB1 (triple variant haplotype, rs1128503), previously associated with ABCB1 and SLCO1B1 SNPs. Several combinations of SLCO1B1 and SLC22A16 with ABCB1 SNPs were associated with higher toxicities, includin…

AdultCancer ResearchGenotypeAnthracyclineSingle-nucleotide polymorphismPolymorphism Single Nucleotide03 medical and health sciences0302 clinical medicineMucositisHumansMedicineIdarubicinAnthracyclinesProspective StudiesbiologyLiver-Specific Organic Anion Transporter 1business.industryHaplotypeInduction chemotherapyMyeloid leukemiaInduction ChemotherapyHematologymedicine.diseaseMultidrug Resistance-Associated Protein 2Leukemia Myeloid AcuteOncology030220 oncology & carcinogenesisbiology.proteinCancer researchATP-Binding Cassette TransportersbusinessSLCO1B1030215 immunologymedicine.drugLeukemia & Lymphoma
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