grant

Biochemical Analysis of Multidrug Resistance-linked Transport Proteins

Organization DIVISION OF BASIC SCIENCES - NCILocation UNITED STATES
NIHUS FederalResearch GrantFY20251H-Purin-6-amineABC Transport ProteinABC Transporter ProteinABC TransportersABC15ABC20ABC29ABCB1ABCB1 geneABCCABCC1ABCC1 geneABCG2ABCG2 geneABCPABL1ABL1 geneATP phosphohydrolaseATP-Binding Cassette TransportersATP-Binding Cassette, Sub-Family G (WHITE), Member 2 GeneATP-Binding Cassette, Sub-Family G, Member 2ATP-Binding Cassette, Subfamily G, Member 2ATPaseAbelson Murine Leukemia Viral Oncogene Homolog 1AdenineAdenosine A3 ReceptorAdenosine ReceptorsAdenosine TriphosphataseAffectAffinityAgonistAnti-Cancer AgentsAntineoplastic AgentsAntineoplastic DrugsAntineoplasticsAreaAssayAtrophic ArthritisBCRPBCRP1BaculoviridaeBaculovirus Expression SystemBaculovirusesBindingBinding SitesBioassayBioavailabilityBiochemicalBiological AssayBiological AvailabilityBreast Cancer Resistance ProteinCancer CauseCancer DrugCancer EtiologyCancer PatientCancer TreatmentCarrier ProteinsCell BodyCell surfaceCellsChemicalsChemoresistanceChemotherapy ProtocolChemotherapy RegimenChemotherapy-Oncologic ProcedureChronic DiseaseChronic IllnessClinicalClinical TrialsCombination Chemotherapy RegimenCombining SiteCommunicationCryo-electron MicroscopyCryoelectron MicroscopyDNA mutationDataDevelopmentDockingDoseDrug EffluxDrug InteractionsDrug KineticsDrug TransportDrug resistanceDrugsEGFR BlockerEGFR InhibitorEGFR Tyrosine Kinase InhibitorEGFR-TK InhibitorERBB2ERBB2 geneEST157481Electron CryomicroscopyEpidermal Growth Factor Receptor InhibitorEpidermal Growth Factor Receptor Tyrosine Kinase InhibitorEthidium BromideExhibitsFDA approvedFormulationGP170GS-XGenetic ChangeGenetic defectGenetic mutationGenetics-MutagenesisGenus HippocampusGoalsHER -2HER-2HER2HER2 GenesHER2/neuHeLaHela CellsHepatocarcinomaHepatocellular CarcinomaHepatocellular cancerHepatomaHomidium BromideHumanIn VitroInsectaInsectsInsects InvertebratesJTK7LeadLibrariesLigandsLightLinkLiver Cells CarcinomaLysolecithinsLysophosphatidylcholinesMDA MB 231MDA-231MDA-MB231MDR-1MDR1MDR1 ProteinMRP1MRXMXR1Malignant CellMalignant Neoplasm TherapyMalignant Neoplasm TreatmentMediatingMedicationMembraneMetabolicMitochondriaMitoxantrone Resistance ProteinModern ManMolecularMolecular ConfigurationMolecular ConformationMolecular Dynamics SimulationMolecular InteractionMolecular Modeling Nucleic Acid BiochemistryMolecular Modeling Protein/Amino Acid BiochemistryMolecular ModelsMolecular StereochemistryMulti-Drug ResistanceMultidrug ResistanceMultidrug Resistance 1Multidrug Resistance Gene-1Multidrug Resistance Gene-1sMultidrug Resistance ProteinsMultidrug Resistant ProteinsMultiple Drug ResistanceMultiple Drug ResistantMutagenesisMutagenesis Molecular BiologyMutationMutation AnalysisNEU OncogeneNEU proteinNIDDKNamesNational Institute of Diabetes and Digestive and Kidney DiseasesNational Institutes of HealthNatural ProductsNeoplastic Disease Chemotherapeutic AgentsNucleosidesNucleotidesOncogene ErbB2OrphanP-GPP-GlycoproteinP-Glycoprotein 1 GeneP1 PurinoceptorsPGY-1 ProteinPGY1PTK InhibitorsPUVAPUVA PhotochemotherapyPatternPb elementPharmaceutical PreparationsPharmacokineticsPhotochemistryPhotochemotherapyPhotodynamic TherapyPhotoradiationPhotosensitizersPhotosensitizing AgentsPhysiologic AvailabilityPlacenta-Specific ATP-Binding Cassette TransporterPlayPrimary carcinoma of the liver cellsProductionPropertyProtein Tyrosine Kinase InhibitorsPsoriasisPurinergic P1 ReceptorsQuimioterapiaReactive SiteReceptor ProteinRegulationResistanceResistance to Multi-drugResistance to MultidrugResistance to Multiple DrugResistant to Multiple DrugResistant to multi-drugResistant to multidrugResolutionRheumatoid ArthritisRhodamine 123RoleSeahorseSiteStructureSubstrate SpecificitySuppressor MutationsTK InhibitorsTKR1TM DomainTNBCTariquidarTestingTherapeuticTimeTransmembrane DomainTransmembrane RegionTransport Protein GeneTransport ProteinsTransporter ProteinTumor-Specific Treatment AgentsTyrosine Kinase InhibitorUnited States National Institutes of HealthVinblastineVincaleucoblastineVincaleukoblastineVitamin B4WorkXenobioticsanti-cancer druganti-cancer therapyc-Ablc-abl Genesc-abl Proto-Oncogenesc-erbB-2c-erbB-2 Genesc-erbB-2 Proto-Oncogenescancer cellcancer chemotherapycancer drug resistancecancer therapycancer-directed therapychemical librarychemoresistantchemotherapy resistancechemotherapy resistantchronic disorderchronic painconformationconformationalconformational stateconformationallyconformationscryo-EMcryoEMcryogenic electron microscopydesigndesigningdevelopmentaldisableddrug repositioningdrug repurposingdrug resistantdrug-sensitivedrug/agenterbB-2 Genesexperimentexperimental researchexperimental studyexperimentsgenome mutationheavy metal Pbheavy metal leadherstatinhygromycinhygromycin Ain silicoinhibitorinnovateinnovationinnovativeinterdisciplinary approachkinase inhibitorliposomal formulationliposomal preparationliver carcinomaluminescencemembrane structuremitochondrialmolecular dynamicsmolecular modelingmulti-drug resistantmulti-drug resistant cancermultidisciplinary approachmultidrug resistantmultidrug resistant cancermutantnamenamednamingnanonaturally occurring productneoplasm/cancer photoradiation therapyneu Genesnew therapeutic approachnew therapeutic interventionnew therapeutic strategiesnew therapy approachesnew treatment approachnew treatment strategynovel therapeutic approachnovel therapeutic interventionnovel therapeutic strategiesnovel therapy approachoverexpressoverexpressionphotosensitizerpsoriasiformpsoriaticreceptorrepurposing agentrepurposing medicationresistance to Drugresistance to cancer drugsresistantresistant to Drugresistant to cancer drugsresolutionsrheumatic arthritisrisk mitigationscreeningscreeningsself assemblysimulationsmall moleculesmall molecule librariessocial rolespatial and temporalspatial temporalspatiotemporalstable cell linesuccesssystemic toxicitytariquidarththermolabilitythermostabilitytriple-negative breast cancertriple-negative invasive breast carcinomauptake
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Description preview

Clinical resistance to multiple chemically and functionally dissimilar drugs is multifaceted. P-glycoprotein (P-gp, ABCB1) and ABCG2 appear to contribute to this problem due to their broad and overlapping substrate specificities. Both transporters also play an important role in drug-drug interactions as well as in the bioavailability and…

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