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Glutathione transporter as a target for brain drug delivery
Inability to achieve therapeutic concentrations of a medication in the brain due to the blood brain barrier (BBB) is the major cause of treatment...
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Plasmodium falciparum: Transporter and Drug Target
Malaria will continue to be a concern for public health well into the future, as it is responsible for more than 50 million fatalities annually...
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Discovery and Development of Monoamine Transporter Ligands
Monoamine transporters (MATs) are targets of a wide range of compounds that have been developed as therapeutic treatments for various...
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Astrocyte Glutamate Transporter EAAT2 in Alzheimer Dementia
Glutamate is an amino acid and also the major synaptic signaling molecule of neurons, essential in cognition, learning, and memory. Glutamate is...
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Effect of Nitric Oxide on the Functioning of the P-Glycoprotein Transporter
We studied the effect of nitric oxide (NO) on the functioning of P-glycoprotein transporter (Pgp) in Caco-2 cells. NO donor S-nitrosoglutathione...
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Transporter Systems and Metabolism at the Blood–Brain Barrier and Blood–CSF Barrier
Neurodegenerative disorders, including Alzheimer’s disease (AD), Parkinson’s disease (PD), and Huntington’s disease (HD), are a leading cause of...
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Interaction of the chemotherapeutic agent oxaliplatin and the tyrosine kinase inhibitor dasatinib with the organic cation transporter 2
Oxaliplatin (OHP) is effective in colorectal cancer treatment but induces peripheral neurotoxicity (OHP-induced peripheral neurotoxicity, OIPN),...
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Vitamin C transporter SVCT1 serves a physiological role as a urate importer: functional analyses and in vivo investigations
Uric acid, the end product of purine metabolism in humans, is crucial because of its anti-oxidant activity and a causal relationship with...
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Characterizing Dopamine Transporter Mediated Uptake and Efflux in Brain Slices: A New Approach
The dopamine transporter (DAT) plays a fundamental role in dopamine (DA) neurotransmission by retrieving the transmitter from the extracellular space...
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Perfluoroalkyl substances (PFASs) are substrates of the renal human organic anion transporter 4 (OAT4)
Poly- and perfluoroalkyl substances (PFASs) are omnipresent in the environment and have been shown to accumulate in humans. Most PFASs are not...
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The ATP-Binding Cassette Transporter-Mediated Efflux Transport of Ganciclovir at the Blood–Brain Barrier
Background and ObjectiveRecent studies have highlighted the key role of the ATP-binding cassette (ABC) transporters, including the P-glycoprotein...
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Characterization of Aripiprazole Uptake Transporter in the Blood-Brain Barrier Model hCMEC/D3 Cells by Targeted siRNA Screening
AimIdentification of blood-brain barrier (BBB) uptake transporters is a major challenge in the research and development of central nervous system...
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Tranilast-tyrosine hybrid molecule exhibits dual activity: suppression of epithelial-mesenchymal transition and induction of cytotoxicity in cancer cells
The anti-allergic drug tranilast (TNL) reportedly exhibits inhibitory activity against epithelial-mesenchymal transition (EMT) at high...
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Cocaine regulates antiretroviral therapy CNS access through pregnane-x receptor-mediated drug transporter and metabolizing enzyme modulation at the blood brain barrier
BackgroundAppropriate interactions between antiretroviral therapies (ART) and drug transporters and metabolizing enzymes at the blood brain barrier...
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Epstein–Barr virus infection controls the concentration of the intracellular antioxidant glutathione by upregulation of the glutamate transporter EAAT3 in tumor cells
Epstein–Barr virus or human herpesvirus 4 (EBV/HHV-4) is an omnipresent oncovirus etiologically associated with various B-cell lymphomas and...
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The landscape of small-molecule prodrugs
Prodrugs are derivatives with superior properties compared with the parent active pharmaceutical ingredient (API), which undergo biotransformation...
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Computational modeling of PET imaging agents for vesicular acetylcholine transporter (VAChT) protein binding affinity: application of 2D-QSAR modeling and molecular docking techniques
The neurotransmitter acetylcholine (ACh) plays a ubiquitous role in cognitive functions including learning and memory with widespread innervation in...
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Blockade of the amino acid transporter SLC6A14 suppresses tumor growth in colorectal Cancer
BackgroundThe amino acid transporter SLC6A14, which transports 18 of the 20 proteinogenic amino acids, is too low to be detected in healthy normal...
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High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3
IntroductionThe organic cation transporter 3 (OCT3, SLC22A3) is ubiquitously expressed and interacts with a wide array of compounds including...
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Downregulation of the glucose transporter GLUT 1 in the cerebral microvasculature contributes to postoperative neurocognitive disorders in aged mice
IntroductionGlucose transporter 1 (GLUT1) is essential for glucose transport into the brain and is predominantly expressed in the cerebral...
