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 23 for “"drug transporters"”.
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Expression and function of drug transporters in primitive CML cells
… Such resistance to classical chemotherapeutic drugs, the phenomenon of multidrug resistance (MDR), is mediated by ABC transporters. In this study we have investigated whether CML SC express the clinically relevant ABC transporters and determine their interaction with TKIs. In addition, we …
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Regulation of Hepatic Drug Transporters Expression in Mice During Acute Inflammation
… and activity of several hepatic ABC and SLC transporters and drug-metabolizing enzymes. These pronounced changes in hepatic transporters contribute to altered drug disposition; therefore, understanding the molecular mechanisms would aid in identifying potential sources of drug variability in …
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Renal Drug Transporters – Clinical Significance and Role in Drug-Drug Interactions
Drug transporters play an important role in drug disposition and can be major determinants of drug pharmacokinetics, pharmacodynamics and toxicity. In contrast to drug metabolizing enzymes, which mainly concentrate in the liver and small intestine, drug transporters are expressed ubiquitously …
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Regulation of Human Renal Drug Transporters by Inflammatory Cytokines and Pregnancy-related Hormones in Primary Proximal Tubular Epithelial Cells
Systemic inflammation and pregnancy both alter drug pharmacokinetics by changing physiology and modulating drug-metabolizing enzymes and transporters in eliminating organs. Regulation of hepatic enzymes in these states is relatively well described. However, the magnitude, direction, and mechanisms …
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PREDICTION OF HUMAN SYSTEMIC, BIOLOGICALLY RELEVANT PHARMACOKINETIC (PK) PROPERTIES BASED ON QUANTITATIVE STRUCTURE PHARMACOKINETIC RELATIONSHIPS (QSPKR) AND INTERSPECIES PHARMACOKINETIC ALLOMETRIC SCALING (PK-AS)
… three, preselected, pharmacological classes of drugs, namely opioids, β-adrenergic receptor ligands (β-ARL) and β-lactam antibiotics (β-LAs) using pertinent human and animal systemic PK properties (fu,, CLtot, Vdss, fe) and their biologically relevant unbound counterparts from the published …
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Role of Membrane Transporters in Drug Delivery, Drug Disposition And Drug-Drug Interactions
… kidney, brain and intestine expresses membrane transporters which play a vital role in drug absorption, distribution, metabolism and excretion. Understanding of functionality and molecular expression of drug transporters can prove to be of utmost importance in drug delivery or drug design by …
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Subcellular Localization and Activity of the Multidrug Resistance Protein 1
<p>Multi-drug resistance or MDR is a major impediment to the successful administration of chemotherapy. Broadly defined, the term MDR applies to any mechanism the cell uses to counter the effects of chemotherapeutic agents, protecting the cell at once against the toxicity of many, structurally …
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Modulation of drug transport by citrus fruit juices
Fruit juice-drug interactions involving drug transporters have been variously studied with citrus fruit juices. The collective data led us to hypothesize that the modulating activity of citrus fruit juices on cellular transport and metabolic pathways is dependent on the dominant flavonoid pattern …
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Equilibrative Nucleoside Transporter Mediated Drug Disposition Across the Blood-Testis Barrier
… of male contraceptives and fertility treatments. Drug transporters present at the basal and apical membranes of testicular epithelial cells (Sertoli cells) facilitate the disposition of therapeutics across the BTB. Many antivirals and chemotherapeutic agents are classified as nucleoside analogs, …
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Characterization and Inhibition of the Dimer Interface in Bacterial Small Multidrug Resistance Proteins
… several families of membrane-embedded α-helical transporters to remove cytotoxic molecules from the cell. The small multidrug resistance protein family (SMR) is one such group of drug transporters that because of their relative small size [ca. 110 residues with four transmembrane (TM) helices] …
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Genetic Predictors of Hyperglycemia Due to Hydrochlorothiazide Therapy
… Some patients respond favorably to a drug while others develop adverse reactions. Early investigations showed evidence of variation in genes that code for drug receptors, drug transporters, and drug metabolizing enzymes; and pharmacogenetics appeared as the science that studies the …
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Regulation and functional significance of ATP binding cassette transporters in human placenta
… project was to study ATP binding cassette (ABC) transporters in the human placenta, in particular their regulation and role in trophoblast differentiation and survival. The presence and localisation of four major placental drug transporters, multidrug resistance gene product 1 and 3 (MDR1 and …
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Drug Metabolizing Enzyme, Drug Transporter Expression And Drug Disposition Are Altered In Models Of Inflammatory Liver Disease
… is based on the idea that too much of a drug will cause toxicity, while too little will result in failure to elicit the desired response. A major factor in the ability of a patient to handle any dose of a drug is the capacity to metabolize and eliminate that drug from the body. For the …
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Nash Alters Drug Metabolizing Enzyme and Transporter Expression Resulting in Significant Consequences for Pharmaceutical Disposition and Toxicity
… The major cellular effectors of ADME are the drug metabolizing enzymes (DMEs) and transporters. DMEs function to transform xenobiotics into a metabolite that is more suitable for excretion, whereas drug transporters serve a two-fold function. They may facilitate the uptake of the xenobiotic …
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Meta-analysis of the population and phenotypic expression of CYP2C9/2C19 polymorphism on drug metabolism in different ethnicities
… study of inherited factors that affect the human drug response. Many pharmacogenetie studies have been published since 1995 and have focussed on the principal enzyme family involved in drug metabolism, the cytochrome P450 family, particularly cytochrome P4502C9 and 2C19. In order to investigate …
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Structural and Mechanistic Studies of Multidrug Resistance Efflux Pumps in Multiple Families
Multidrug resistance, whereby pathogens develop resistance to several antimicrobial agents, is a large and growing public health concern globally. In order to combat its continued spread, a better understanding of resistance mechanisms is necessary. One recurring mechanism of multidrug resistance …
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Subcellular Fractionation Methods for the Quantification of Endogenous Protein in Human Liver Using Targeted Proteomics
… spectrometry method with many applications in drug development. Due to its high selectivity, fast analysis time and high sensitivity, UPLC-MRM is widely used in sample bioanalysis for pharmacokinetics. Recently, interest into human endogenous protein quantification using targeted quantitative …
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Energetics and Structural Aspects of Cation-Coupled Drug Transport by NorM Multidrug Transporters
NorM multidrug transport proteins belong to the multiple antibiotics and toxins extrusion (MATE) family of secondary active transporters. Members of this family are present across all species including bacteria, plants and humans. In bacteria, their over-expression can lead to antibiotic …
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Functional Expression of ABC Transporters at Blood-tissue Barriers: Relevance to Antiretroviral Drug Tissue Distribution
… several studies have observed antiretroviral drugs present at sub-therapeutic concentrations in these tissue compartments that may contribute to the formation of drug resistance and allow systemic viral repopulation. ATP-binding cassette drug efflux transporters i.e., P-glycoprotein and breast …
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