Sökning: "free drug"

Visar resultat 1 - 5 av 308 avhandlingar innehållade orden free drug.

  1. 1. Intracellular unbound drug concentrations : Methodology and application for understanding cellular drug exposure

    Författare :André Mateus; Per Artursson; Pär Matsson; José A. G. Morais; Jeff Krise; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; intracellular unbound drug concentrations; free drug; drug binding; drug transport; drug accumulation; cellular drug response; drug target engagement; Pharmaceutical Science; Farmaceutisk vetenskap;

    Sammanfattning : Most known drug targets and metabolizing enzymes are located inside cells. Interactions with these proteins are determined by intracellular unbound drug concentrations. Assessing intracellular drug exposure is technically challenging, but essential for predicting pharmacokinetic, pharmacological, and toxicological profiles of new drugs. LÄS MER

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

    Författare :Andrea Treyer; Per Artursson; Gert Fricker; Uppsala universitet; []
    Nyckelord :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;

    Sammanfattning : 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. LÄS MER

  3. 3. Drug absorption in the lungs : studies in the isolated perfused rat lung model combined with physiologically based biopharmaceutics modelling

    Författare :Johanna Eriksson; Hans Lennernäs; Erik Sjögren; Helena Thörn; Ben Forbes; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pulmonary drug absorption; physiologically based biopharmaceutics modeling; pulmonary drug delivery; Biofarmaci; Biopharmaceutics;

    Sammanfattning : Pulmonary delivery of drugs is the preferred route of administration for treatment of local lung diseases like asthma and chronic obstructive pulmonary disease. Recently, there has also been increased interest in systemic delivery of drugs via the lungs to avoid problems with low and/or variable gastrointestinal absorption, and as a needle-free alternative for drugs that cannot be ingested. LÄS MER

  4. 4. Algorithmic discovery, development and personalized selection of higher-order drug cocktails : A label-free live-cell imaging & secretomics approach

    Författare :Efthymia Chantzi; Mats G Gustafsson; Ulf Hammerling; Andreas Bender; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; drug combination discovery and development; personalized pharmacotherapy; higher-order drug combination analysis; quantitative label-free live-cell imaging; secretomics; cell-cell communication; deep learning; convolutional neural networks; data mining; MapReduce; resampling; generalized highest single agent; COMBImageDL; COMBSecretomics; Bioinformatics; Bioinformatik; Pharmacology; Farmakologi; Engineering Science; Teknisk fysik;

    Sammanfattning : An upward trend in clinical pharmacology is the use of multiple drugs to combat complex and co-occurring diseases due to better efficacy, decreased toxicity and reduced risk of evolving resistance. Despite high late-stage attrition rates and the need for multi drug treatments, most drug discovery and development efforts are still mainly focused on new one-size-fits-all monotherapies. LÄS MER

  5. 5. Free-energy studies of ligand-binding affinities

    Författare :Vilhelm Ekberg; Beräkningskemi; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; free energy perturbation; drug design; ligand-binding affinity; entropy; molecular mechanics; molecular dynamics;

    Sammanfattning : In drug discovery, it is of utmost importance to accurately calculate the free energies of binding ligands to various protein targets, such as enzymes and receptors. We have assessed and used computational tools for this aim, most of them based on molecular dynamics (MD) simulations. LÄS MER