Search results for " ATP-binding cassette"

showing 4 items of 4 documents

Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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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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Decreasing dietary linoleic acid promotes long chain omega-3 fatty acid incorporation into rat retina and modifies gene expression

2011

International audience; Age-related macular degeneration (AMD) may be partially prevented by dietary habits privileging the consumption of ω3 long chain polyunsaturated fatty acids (ω3s) while lowering linoleic acid (LA) intake. The present study aimed to document whether following these epidemiological guidelines would enrich the neurosensory retina and RPE with ω3s and modulate gene expression in the neurosensory retina. Rat progenitors and pups were fed with diets containing low or high LA, and low or high ω3s. After scotopic single flash and 8-Hz-Flicker electroretinography, rat pups were euthanized at adulthood. The fatty acid profile of the neurosensory retina, RPE, liver, adipose tis…

CD36 AntigensMaleMESH : RNA MessengerMESH: 5-Lipoxygenase-Activating ProteinsMESH : Receptors LDLMESH: Electroretinography0302 clinical medicineMESH: Fatty Acids Omega-3MESH: AnimalsMESH : Retinal Ganglion Cellschemistry.chemical_classification0303 health sciencesMESH : Gene Expression RegulationMESH : ElectroretinographyMESH: RetinaMESH: Chromatography GasMESH: Dietary Fats Unsaturateddocosahexaenoic acidpolyunsaturated fatty acidSensory Systems3. Good healthnutritionMESH: Photic StimulationAdipose TissueMESH: Adipose Tissuemedicine.medical_specialtyChromatography Gasmacular degenerationLinoleic acidMESH : Arachidonate 12-LipoxygenaseArachidonate 12-LipoxygenaseMESH : Adipose TissueMESH: Arachidonate 12-Lipoxygenasepufa03 medical and health sciencesMESH : Dietary Fats UnsaturatedlipidElectroretinographyRats Long-EvansRNA MessengerMESH: Linoleic AcidMESH: Antigens CD36MESH : RetinaFatty acidMESH: Retinal Ganglion Cellseye diseasesOphthalmologyEndocrinologychemistryMESH: Receptors LDL030221 ophthalmology & optometryATP-Binding Cassette Transportersn 3MESH: FemalePhotic StimulationMESH: LiverRetinal Ganglion CellsretinaMESH : 5-Lipoxygenase-Activating Proteinsgenetic structures[ SDV.AEN ] Life Sciences [q-bio]/Food and Nutritionretinal pigment epitheliumelectroretinogramMESH : Photic StimulationAdipose tissueangiogenesischemistry.chemical_compoundMESH : FemaleMESH : Rats Long-Evans2. Zero hungermedicine.diagnostic_testMESH : RatsMESH: Real-Time Polymerase Chain ReactionMESH: Gene Expression RegulationMESH : Antigens CD36medicine.anatomical_structureLiverALOX12BiochemistryMESH: ATP-Binding Cassette TransportersFemaleATP Binding Cassette Transporter 1Polyunsaturated fatty acidMESH : Fatty Acids Omega-3MESH: RatsbrainMESH : Male5-Lipoxygenase-Activating ProteinsMESH : Real-Time Polymerase Chain Reactionrhesus monkeyBiologyReal-Time Polymerase Chain ReactionMESH : Chromatography GasLinoleic AcidCellular and Molecular NeuroscienceDietary Fats UnsaturatedMESH : Linoleic AcidMESH: Rats Long-EvansInternal medicineFatty Acids Omega-3medicineAnimalsMESH : ATP-Binding Cassette TransportersOmega 3 fatty acidMESH: RNA Messenger030304 developmental biologydeficient dietRetinal pigment epitheliumMESH : LiverMESH: MaleRatsGene Expression RegulationReceptors LDLgene expressionMESH : Animalssense organs[SDV.AEN]Life Sciences [q-bio]/Food and NutritionElectroretinographyExperimental Eye Research
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Peroxisomal and mitochondrial status of two murine oligodendrocytic cell lines (158N, 158JP): potential models for the study of peroxisomal disorders…

2009

International audience; In some neurodegenerative disorders (leukodystrophies) characterized by myelin alterations, the defect of peroxisomal functions on myelin-producing cells (oligodendrocytes) are poorly understood. The development of in vitro models is fundamental to understanding the physiopathogenesis of these diseases. We characterized two immortalized murine oligodendrocyte cell lines: a normal (158N) and a jimpy (158JP) cell line mutated for the proteolipid protein PLP/DM20. Fluorescence microscopy, flow cytometry, and western blotting analysis allow to identify major myelin proteins (PLP colocalizing with mitochondria; myelin basic protein), oligodendrocyte (CNPase and myelin oli…

Proteolipid protein 1BiochemistryMiceMyelinMESH : PhenylbutyratesperoxisomeIsomerasesMESH : Myelin Basic ProteinsEnoyl-CoA HydrataseCell Line TransformedUltrasonographybiologyMESH : Gene Expression RegulationMESH : Myelin Proteolipid Protein3-Hydroxyacyl CoA DehydrogenasesMESH : Myelin-Associated GlycoproteinMESH : Cell Line TransformedPeroxisomeMESH : Multienzyme ComplexesMESH : OligodendrogliaMESH : Enoyl-CoA HydrataseCatalaseFlow CytometryMESH : 3-Hydroxyacyl CoA DehydrogenasesPhenylbutyratesmitochondriaMyelin-Associated GlycoproteinOligodendrogliamyelinMESH : Antineoplastic Agentsmedicine.anatomical_structureMESH : Microscopy Electron TransmissionBiochemistryACOX1MESH : MitochondriaMESH : Acyl-CoA Oxidase2'3'-Cyclic-Nucleotide PhosphodiesterasesMESH : IsomerasesOxidation-ReductionMyelin ProteinsMESH : Flow CytometryAntineoplastic AgentsPeroxisomal Bifunctional EnzymeStatistics NonparametricMyelin oligodendrocyte glycoproteinCellular and Molecular NeuroscienceMicroscopy Electron TransmissionMultienzyme ComplexesMESH : CatalaseMESH : MicePeroxisomesmedicineAnimalsMESH : ATP-Binding Cassette TransportersMyelin Proteolipid ProteinMESH : Statistics Nonparametric[ SDV.BBM ] Life Sciences [q-bio]/Biochemistry Molecular BiologyMESH : Oxidation-ReductionMyelin Basic Proteinmurine oligodendrocytesMESH : 2'3'-Cyclic-Nucleotide PhosphodiesterasesPeroxisomal transportOligodendrocyteMyelin basic proteinGene Expression Regulationbiology.proteinATP-Binding Cassette TransportersMyelin-Oligodendrocyte GlycoproteinAcyl-CoA OxidaseMESH : AnimalsMESH : Peroxisomes
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