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Pharmacokinetic Modeling of the Effect of Tariquidar on Ondansetron Disposition into the Central Nervous System
PurposeSerotonin (5-HT 3 ) receptor antagonists are promising agents for treatment of neuropathic pain. However, insufficient drug exposure at the...
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Development of core–shell structured nanoparticle for sequential release of tariquidar and docetaxel to overcome multi drug-resistant cancer
PurposeWe developed a core–shell (CS) nanoparticle, docetaxel (DTX)-loaded core and tariquidar (TRQ)-loaded shell conjugated with PEG and RIPL...
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Acyclovir Brain Disposition: Interactions with P-gp, Bcrp, Mrp2, and Oat3 at the Blood–Brain Barrier
Background and ObjectiveAcyclovir is effective in treating herpes simplex virus infections of the central nervous system. The purpose of this study...
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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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Molecular docking study of lignanamides from Cannabis sativa against P-glycoprotein
P-glycoprotein (P-gp), which was first identified in cancer cells, is an ATP-dependent efflux transporter that expels a wide variety of cytotoxic...
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Modulating P-glycoprotein Regulation as a Therapeutic Strategy for Pharmacoresistant Epilepsy
Experimental data suggest a role of blood–brain barrier P-glycoproteinP-glycoprotein (P-gp) overexpression as a factor contributing to drug-resistant...
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CD30 and ALK combination therapy has high therapeutic potency in RANBP2-ALK-rearranged epithelioid inflammatory myofibroblastic sarcoma
BackgroundEpithelioid inflammatory myofibroblastic sarcoma (eIMS) is characterised by perinuclear ALK localisation, CD30 expression and early relapse...
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Abcg2a is the functional homolog of human ABCG2 expressed at the zebrafish blood–brain barrier
BackgroundA principal protective component of the mammalian blood–brain barrier (BBB) is the high expression of the multidrug efflux transporters...
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Advances in the structure, mechanism and targeting of chemoresistance-linked ABC transporters
Cancer cells frequently display intrinsic or acquired resistance to chemically diverse anticancer drugs, limiting therapeutic success. Among the main...
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Knockout Transporter Cell Lines to Assess Substrate Potential Towards Efflux Transporters
P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance transporter 2 (MRP2) are efflux transporters involved in the...
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Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration
Background and objectiveP-glycoprotein (P-gp), a transmembrane transporter expressed at the blood–brain barrier, restricts the distribution of...
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Targeted CRISPR activation and knockout screenings identify novel doxorubicin transporters
PurposeTissue-specific drug uptake has not been well studied, compared to the deeper understanding of drug resistance mediated by the cellular efflux...
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PET imaging of P2X7R in the experimental autoimmune encephalomyelitis model of multiple sclerosis using [11C]SMW139
BackgroundNon-invasive imaging of the activation status of microglia and the ability to identify a pro- or anti-inflammatory environment can provide...
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Similarities and differences in the localization, trafficking, and function of P-glycoprotein in MDR1-EGFP-transduced rat versus human brain capillary endothelial cell lines
BackgroundIn vitro models based on brain capillary endothelial cells (BCECs) are among the most versatile tools in blood–brain barrier research for...
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Recent Development of Quinoline Derivatives as Anticancer Agents: 2015–2022
Increased rate of emergence of cancer cases has led to increased demand of new molecules that have low toxicity profile and high efficiency....
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Strategies for enhanced bioavailability of oxime reactivators in the central nervous system
Oxime reactivators of acetylcholinesterase are commonly used to treat highly toxic organophosphate poisoning. They are effective nucleophiles that...
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Polymeric Nanoparticles that Entrap Drug Combinations Targeted to Solid Tumors
Cancer causes millions of deaths. Cancer occurs in almost any body organ when abnormal cells grow rapidly and spread to other tissues and organs....
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Ligand Targeted Polymeric Nanoparticles for Cancer Chemotherapy
Cancer induces various types of tumors that affects every body part. Effective cancer-targeted therapy involves the use of site-specific drugs...
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Nanomedicine Targeting Cancer Stem Cells
Cancer stem cells (CSCs) constitute a subset of cells endowed with the remarkable abilities of self-renewal, proliferation, and differentiation....
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The role of mutations associated with familial neurodegenerative disorders on blood–brain barrier function in an iPSC model
BackgroundBlood–brain barrier dysfunction is associated with many late-stage neurodegenerative diseases. An emerging question is whether the...
