Search for dissertations about: "ADME"

Showing result 1 - 5 of 8 swedish dissertations containing the word ADME.

  1. 1. Exploring Inhibitors of HIV-1 Protease : Interaction Studies with Applications for Drug Discovery

    Author : Maria T. Lindgren; Helena Danielson; Jozsef Tözser; Uppsala universitet; []
    Keywords : NATURAL SCIENCES; NATURVETENSKAP; NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; kinetics; biosensors; ADME; drug discovery; SPR; resistance; inhibition; copper; Biokemi; Biochemistry; Biokemi;

    Abstract : A variety of HIV-1 protease inhibitors and their interactions with the enzyme have been characterized in order to identify novel and improved drugs against AIDS. The investigated inhibitors were represented by clinical and non-clinical inhibitors, active site and allosteric inhibitors, transition-state analogues and metal-ions. READ MORE

  2. 2. Characterization of parameters influencing intracellular bioavailability and prediction of intracellular drug exposure

    Author : Andrea Treyer; Per Artursson; Gert Fricker; Uppsala universitet; []
    Keywords : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; intracellular drug bioavailability; unbound drug concentration; drug disposition; ADME; drug transport; drug metabolism membrane partitioning; phospholipid; drug-drug interaction; antisense oligonucleotide; cell-penetrating peptide; Farmaceutisk vetenskap; Pharmaceutical Science;

    Abstract : This thesis work investigates factors influencing intracellular drug disposition. An experimental method for measurement of intracellular bioavailability (Fic), was used throughout. Fic is defined as the ratio between the unbound drug concentration inside the cell and the compound concentration in the cell exterior. READ MORE

  3. 3. Proteomics informed investigation of human hepatocytes and liver tissue

    Author : Niklas Handin; Per Artursson; Peter Nygren; Tobias Sjöblom; Mårten Fryknäs; Pieter Annaert; Uppsala universitet; []
    Keywords : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; human; liver; hepatocytes; proteomics; cellular stress; apoptosis; hepatotoxicity; 3D culture; spheroid; drug metabolism; drug toxicity; drug transport; Farmaceutisk vetenskap; Pharmaceutical Science;

    Abstract : A successful drug needs to display beneficial absorption, distribution, metabolism, excretion and toxicity (ADME-Tox) profile. It is therefore important to investigate these properties during the drug discovery process. READ MORE

  4. 4. Proteomic and Functional Analysis of In Vitro Systems for Studies of Drug Disposition in the Human Small Intestine and Liver

    Author : Magnus Ölander; Per Artursson; Pär Matsson; Edward L. LeCluyse; Volker Lauschke; Uppsala universitet; []
    Keywords : MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; proteomics; drug disposition; ADMET; drug transport; drug metabolism; hepatotoxicity; small intestine; liver; caco-2; human hepatocytes; cryopreservation; apoptosis; liver zonation; non-parenchymal cells; Farmaceutisk vetenskap; Pharmaceutical Science;

    Abstract : To reach the bloodstream, an orally administered drug must be absorbed through the small intestine and avoid extensive clearance in the liver. Estimating these parameters in vitro is therefore important in drug discovery and development. READ MORE

  5. 5. Towards Mosquitocides for Prevention of Vector-Borne Infectious Diseases : discovery and Development of Acetylcholinesterase 1 Inhibitors

    Author : Sofie Knutsson; Anna Linusson; Fredrik Almqvist; Andreas Larsson; Ulf Nilsson; Umeå universitet; []
    Keywords : NATURAL SCIENCES; NATURVETENSKAP; NATURVETENSKAP; NATURAL SCIENCES; Mosquito; vector-borne diseases; vector control; insecticide; acetylcholinesterase; medicinal chemistry; high-throughput screening; organic synthesis; homology modeling; structure activity relationship; structure selectivity relationship; datorlingvistik; computational linguistics; organisk kemi; Organic Chemistry;

    Abstract : Diseases such as malaria and dengue impose great economic burdens and are a serious threat to public health, with young children being among the worst affected. These diseases are transmitted by mosquitoes, also called disease vectors, which are able to transmit both parasitic and viral infections. READ MORE