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Extracts from Argentinian native plants reverse fluconazole resistance in Candida species by inhibiting the efflux transporters Mdr1 and Cdr1
BackgroundThe development of multidrug resistance (MDR) associated with the overexpression of the efflux transporters Mdr1 and Cdr1 in Candida ...
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Polymorphic renal transporters and cisplatin’s toxicity in urinary bladder cancer patients: current perspectives and future directions
Urinary bladder cancer (UBC) holds a potentially profound social burden and affects over 573,278 new cases annually. The disease’s primary risk...
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Behaviorally penetrant, anomalous dopamine efflux exposes sex and circuit dependent regulation of dopamine transporters
Virtually all neuropsychiatric disorders display sex differences in prevalence, age of onset, and/or clinical symptomology. Although altered dopamine...
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Nutrient transporters: connecting cancer metabolism to therapeutic opportunities
Cancer cells rely on certain extracellular nutrients to sustain their metabolism and growth. Solute carrier (SLC) transporters enable cells to...
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Combination of mangiferin and T0901317 targeting autophagy promotes cholesterol efflux from macrophage foam cell in atherosclerosis
BackgroundThe synthetic liver X receptor ligand (LXR) T0901317 (T0) has been reported to attenuate atherosclerosis (AS) without hyperglyceridemia due...
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Utilising Endogenous Biomarkers in Drug Development to Streamline the Assessment of Drug–Drug Interactions Mediated by Renal Transporters: A Pharmaceutical Industry Perspective
The renal secretion of many drugs is facilitated by membrane transporters, including organic cation transporter 2, multidrug and toxin extrusion...
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New uracil analog as inhibitor/modulator of ABC transporters or/and NF-κB in taxol-resistant MCF-7/Tx cell line
PurposeThe global increase in breast cancer cases necessitates ongoing exploration of advanced therapies. Taxol (Tx), an initial breast cancer...
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Blocking of efflux transporters in rats improves translational validation of brain radioligands
BackgroundPositron emission tomography (PET) is a molecular imaging technique that can be used to investigate the in vivo pharmacology of drugs....
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Visualizing GABA transporters in vivo: an overview of reported radioligands and future directions
By clearing GABA from the synaptic cleft, GABA transporters (GATs) play an essential role in inhibitory neurotransmission. Consequently, in vivo...
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Zinc transporters ZIPT-2.4 and ZIPT-15 are required for normal C. elegans fecundity
PurposeThe requirement of zinc for the development and maturation of germ lines and reproductive systems is deeply conserved across evolution. The...
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Inhibition of the uric acid efflux transporter ABCG2 enhances stimulating effect of soluble uric acid on IL-1β production in murine macrophage-like J774.1 cells
Soluble uric acid (UA) absorbed by cells through UA transporters (UATs) accumulates intracellularly, activates the NLRP3 inflammasome and thereby...
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Histopathological Features of Pendred Syndrome Thyroids Align with Differences in the Expression of Thyroid-Specific Markers, Apical Iodide Transporters, and Ciliogenesis Process
Pendred syndrome (PDS) is an autosomal recessive disorder caused by mutations in the gene that encodes pendrin. Pendred thyroid tissue is supposedly...
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The influence of verapamil on the pharmacokinetics of the pan-HER tyrosine kinase inhibitor neratinib in rats: the role of P-glycoprotein-mediated efflux
Neratinib, an irreversible pan-HER tyrosine kinase inhibitor, has been approved for the treatment of HER2-positive (HER2 + ) early-stage and brain...
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HDL functionality in type 1 diabetes: enhancement of cholesterol efflux capacity in relationship with decreased HDL carbamylation after improvement of glycemic control
BackgroundReduced cholesterol efflux capacity (CEC) of HDLs is likely to increase cardiovascular risk in type 1 diabetes (T1D). We aimed to assess...
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Luteolin increases susceptibility to macrolides by inhibiting MsrA efflux pump in Trueperella pyogenes
Trueperella pyogenes ( T. pyogenes ) is an opportunistic pathogen associated with a variety of diseases in many domestic animals. Therapeutic treatment...
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Mechanisms and Clinical Significance of Pharmacokinetic Drug Interactions Mediated by FDA and EMA-approved Hepatitis C Direct-Acting Antiviral Agents
The treatment of patients infected with the hepatitis C virus (HCV) has been revolutionised by the development of direct-acting antiviral agents...
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Effects of polymorphisms in pregnane X receptor and ABC transporters on afatinib in Japanese patients with non-small cell lung cancer: pharmacogenomic–pharmacokinetic and exposure–response analysis
PurposeBecause of the large interindividual variability of afatinib pharmacokinetics and adverse events, we evaluated the effects of polymorphisms in...
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Evaluation of ABT-751, a novel anti-mitotic agent able to overcome multi-drug resistance, in melanoma cells
PurposeDrug efflux transporter associated multi-drug resistance (MDR) is a potential limitation in the use of taxane chemotherapies for the treatment...
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Strategies to Combat Bacterial Antimicrobial Resistance: a Focus on Mechanism of the Efflux Pumps Inhibitors
The surge in multidrug resistance (MDR) in the bacterial system has constricted the use of foregoing therapeutics for the treatment of fatal...
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Prediction of drug–drug interaction potential mediated by transporters between dasatinib and metformin, pravastatin, and rosuvastatin using physiologically based pharmacokinetic modeling
PurposeRecent in vitro studies demonstrated that dasatinib inhibits organic cation transporter 2 (OCT2), multidrug and toxin extrusion proteins...
