Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 73 for “"P-gp"”.
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Unbiased assessment of P-gp efflux towards designing blood—brain barrier penetrant compounds
The student, Aya Kelly, accepted the attached license on 2022-04-15 at 10:24.
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Design and evaluation of novel PET and SPECT tracers for imaging the monoamine system and the P-gp transporter
… elements, being the monoamine system and the P-gp transporter, were developed and evaluated in vivo. The first objective of this thesis was the design of radiotracers for the monoamine system more specifically, the norepinephrine transporter, monoamine oxidase and dopamine transporter which are …
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Characterization of P-glycoprotein expression as a multixenobiotic resistance mechanism in fish
Transmembrane P-glycoproteins (P-gps) are responsible for multidrug resistance (MDR) phenotypes in tumor cell lines. P-glycoproteins function as energy dependent efflux flippases that prevent the cellular accumulation of a wide variety of compounds. We characterized P-gp expression in populations …
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Placental P-glycoprotein: Role in disposition of medications administered during pregnancy
… placental efflux transporter P-glycoprotein (P-gp) and its role in regulating the placental distribution of medications used during pregnancy. P-gp expression and transport activity were defined in brush border membrane vesicles prepared from human placenta of various gestational ages. The …
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NSAIDs Modulate Morphine Transport at the Blood-Brain Barrier: A Role for P-glycoprotein
… efflux transporter P-glycoprotein (P-gp) that is endogenously expressed at the blood-brain barrier (BBB). Increased P-gp functional expression was associated with a significant reduction in CNS uptake of morphine and, subsequently, reduced morphine analgesic efficacy. The present study …
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Bioenergetic coupling in P-glycoprotein: determining the relative position, topography and role of transmembrane helices six and twelve
Multidrug efflux pump P-glycoprotein (P-gp) has been the subject of significant research interest since the discovery of the protein in multi-drug resistant cancer cells 40 years ago. Overexpression of P-gp can confer resistance to a broad range of structurally and functionally distinct drugs. The …
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Bioenergetic coupling in P-glycoprotein: determining the relative position, topography and role of transmembrane helices six and twelve
Multidrug efflux pump P-glycoprotein (P-gp) has been the subject of significant research interest since the discovery of the protein in multi-drug resistant cancer cells 40 years ago. Overexpression of P-gp can confer resistance to a broad range of structurally and functionally distinct drugs. The …
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Understanding the Mechanism of Action of Rituximab in the Reversal of Multidrug Resistance in a Non-Hodgkins Lymphoma Cell Line
… stability and organization. P-glycoprotein (P-gp) is the constituent protein of MDR tumor cells and is responsible for pumping chemotherapeutic agents out of cells. Because ~40% of P-gp is contained in lipid rafts, we hypothesized that when CD20 translocated into lipid rafts, it would displace …
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The Role of Astrocyte-Derived Factors in the Regulation of Multidrug Resistance at the Developing Blood-Brain Barrier
P-glycoprotein (P-gp; encoded by Abcb1) at the blood-brain barrier (BBB) plays an important role in regulating the movement of exogenous and endogenous substrates into the developing brain. P-gp levels in brain endothelial cells (BECs), which form the capillaries of the BBB, increase dramatically …
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Docetaxel uptake and modulation of P-gpmediated docetaxel efflux by tyrosine kinase inhibitors in human lung carcinoma cell lines
… of multi-drug resistance (MDR) mediated by P-gp (MDR-1, ABCB1), which is an effective cellular efflux pump for both agents. This thesis was undertaken to examine the contribution of drug transport mechanisms to chemotherapeutic drug resistance, focussing on docetaxel. Sensitive and resistant …
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Characterisation and modulation of drug resistance in lung cancer cell lines
… drug efflux pumps such as P-glycoprotein (P-gp). Using cellular models, this thesis aimed to investigate resistance in lung cancer cells while developing siRNA and membrane proteomic techniques and to increase our knowledge of the effect of lapatinib, a newly developed targeted therapy, in …
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Biopharmaceutical approaches for improved drug delivery across ocular barriers
… compounds. Additionally, P-glycoprotein (P-gp) expressed on the retinal pigmented epithelium (RPE P-gp) limits the penetration of substrates, in therapeutically relevant concentrations, into the back-of-the-eye. </p> <p>In the present research, use of penetration enhancers (chitosan, …
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The influence of genetic polymorphisms and natural health products on drug metabolism
… involved in drug metabolism, P-glycoprotein (P-gp) and members of the cytochrome P450 oxidase (CYP) family were studied. This investigation specifically examined the influence of polymorphisms within the ABCB1 gene on P-gp efflux activity and expression. Additionally, the role of natural health …
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Genetic Determinants of ABCB1 Promoter Activity and Their Effects on Environmental Exposure
… A major placental efflux transporter is P-gp, which is encoded by the ABCB1 gene. Many medications prescribed to pregnant women, such as antibiotics for acute illness or medications used to treat chronic diseases including asthma and diabetes, are P-gp substrates. Variability in placental …
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Intestinal absorption barriers as modelled by p-glycoprotein and cytochrome p450 a34 in caco2 cells
… American Type Tissue Culture collection. High P-gp expressing Caco-2 cells have been developed through stepwise selection of the cells with doxonibicin. This newly-developed cell line (hereafter referred to as Type I) possesses approximately twice as much P-gp protein than non-exposed cells, …
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Role of the Vitamin D Receptor in MDR1/P-glycoprotein Regulation at the Blood-brain Barrier
… the luminal membrane, notably P-glycoprotein (P-gp). It has also been shown that amyloid-β (Aβ), a key player in Alzheimer's disease, is a P-gp substrate. We demonstrate that P-gp levels and function are upregulated upon activation by the vitamin D receptor (VDR) via its natural ligand …
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Pharmacological modulation and manipulation of cancer drug resistance
… assays for their ability to overcome MRP1 and P-gp-mediated drug resistance. Two compounds were successful P-gp modulators in the DLKP-A cell line; the ditrifluoroacetyl resveratrol derivative, RBM15, and the macrocycle derivative, KG104. A panel of nine therapeutic agents were evaluated for …
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Regulation of P-glycoprotein at the Blood-Brain Barrier
… ATP-driven efflux transporter, P-glycoprotein (P-gp) that denies CNS entry to a myriad of therapeutics. Thus, a better understanding of the mechanisms regulating P-gp expression and transport function might provide new strategies to improve drug delivery to the brain and increase drug levels in …
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The relationship between p53 mutations and differential sensitivity to anti-cancer drugs in oesophageal cancer cell lines
… anti-cancer drugs, presence of P-glycoprotein (P-gp) and glutathione-S-transferase (GST), and p53 mutations were investigated. Chemosensitivity of the WHCO1, WHC03 and HCu-13 cell lines to 7 anti-cancer agents was determined. WHC03 was relatively resistant to cisplatin and transplatin, but …
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To Investigate The Impact Of Gut Bacteria On Efflux Transporter Expression And Function In Gastrointestinal Mucosae
… characterize the function of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) using intestinal organoids derived from germ free and humanized mice. Typically, transport across the epithelial cell layers occurs by active transport and passive diffusion. Using mouse models that …
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