Sökning: "ABC transporters"

Visar resultat 1 - 5 av 17 avhandlingar innehållade orden ABC transporters.

  1. 1. In vivo Pharmacokinetics of Two New Thrombin Inhibitor Prodrugs : Emphasis on Intestinal and Hepatobiliary Disposition and the Influence of Interacting Drugs

    Författare :Elin Matsson; Hans Lennernäs; Lars Knutson; Ulf Eriksson; Kim Brouwer; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Direct thrombin inhibitors; prodrugs; ximelagatran; AZD0837; erythromycin; ketoconazole; drug-drug interactions; hepatobiliary transport; biliary clearance; ATP-binding cassette; ABC transporters; solute carriers; SLC transporters; CYP3A4; Biopharmacy; Biofarmaci; Biopharmaceutics; Biofarmaci;

    Sammanfattning : Biliary excretion is an important elimination route for many drugs and metabolites. For such compounds, it is important to know the extent of excretion and drug exposure in the bile, e.g., for the risk assessment of drug interactions, liver toxicity and the effects of genetic variants. LÄS MER

  2. 2. The role of ABC transporters and inflammation in drug-resistant epilepsy

    Författare :Lora Deuitch Weidner; Karolinska Institutet; Karolinska Institutet; []
    Nyckelord :;

    Sammanfattning : This thesis explores two pathologies thought to be related to drug resistance in epilepsy that may themselves be causally related: 1) overexpression of drug transporters in capillaries and 2) inflammation. With regard to the first hypothesis, overexpression of the ATP-binding cassette (ABC) transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), at the blood-brain barrier are thought to contribute to drug resistance in epilepsy. LÄS MER

  3. 3. Intestinal barriers to oral drug absorption: Cytochrome P450 3A and ABC-transport proteins

    Författare :Helena Engman; Per Artursson; Hans Lenernäs; Heyo K Kroemer; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutics; oral drug delivery; bioavailability; human jejunum; Caco-2; ABC-transporter; P-glycoprotein; CYP3A; Galenisk farmaci; Pharmaceutics; Galenisk farmaci;

    Sammanfattning : The subject of this thesis was to study two intestinal barriers to oral drug bioavailability, drug efflux proteins of the ABC-transporter family, and in particular ABCB1/P-glycoprotein (Pgp), and the drug metabolizing enzyme cytochrome P450 (CYP) 3A4. At the onset of this thesis, similarities between CYP3A4 and Pgp in terms of their tissue distribution and gene regulation, along with overlapping substrate specificities, had generated the hypothesis that CYP3A4 and Pgp may have a complementary function and thus form a coordinated intestinal barrier to drug absorption and gut wall metabolism. LÄS MER

  4. 4. ATP-Binding Cassette Efflux Transporters and Passive Membrane Permeability in Drug Absorption and Disposition

    Författare :Pär Matsson; Per Artursson; Ulf Norinder; Peter Swaan; Uppsala universitet; []
    Nyckelord :Pharmaceutics; ATP-binding cassette; ABC transporter; P-gp; P-glycoprotein; ABCB1; BCRP; Breast cancer resistance protein; ABCG2; MRP2; Multidrug-resistance associated protein 2; ABCC2; Membrane permeability; Drug transport; Active transport; Passive diffusion; Multivariate data analysis; PLS; OPLS; QSAR; Galenisk farmaci;

    Sammanfattning : Transport into and across the cells of the human body is a prerequisite for the pharmacological action of drugs. Passive membrane permeability and active transport mechanisms are major determinants of the intestinal absorption of drugs, as well as of the distribution to target tissues and the subsequent metabolism and excretion from the body. LÄS MER

  5. 5. ATP-Binding-Cassette Transporters in Biliary Efflux and Drug-Induced Liver Injury

    Författare :Jenny M. Pedersen; Per Artursson; Christel A. S. Bergström; Stefan Oswald; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; ABC transport protein; Pgp; P-glycoprotein; ABCB1; BCRP; breast cancer resistance protein; ABCG2; MRP2; multidrug resistance-associated protein 2; ABCC2; BSEP; bile salt export pump; ABCB11; sandwich cultured human hepatocytes; SCHH; drug-induced liver injury; DILI; multivariate data analysis; OPLS; Galenisk farmaci; Pharmaceutics;

    Sammanfattning : Membrane transport proteins are known to influence the absorption, distribution, metabolism, excretion and toxicity (ADMET) of drugs. At the onset of this thesis work, only a few structure-activity models, in general describing P-glycoprotein (Pgp/ABCB1) interactions, were developed using small datasets with little structural diversity. LÄS MER