Sökning: "drug binding"

Visar resultat 1 - 5 av 511 avhandlingar innehållade orden drug binding.

  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. Quantum Chemical Studies of Chemotherapeutic Drug Cisplatin : Activation and Binding to DNA

    Författare :Johan Raber; David van der Spoel; Paolo Carloni; Uppsala universitet; []
    Nyckelord :Quantum chemistry; cisplatin; quantum chemistry; DNA; density functional theory; activation; JM118; substitution reaction; Platinum; guanine; adenine; cytostatic drug; aquation; anation; activation; Kvantkemi;

    Sammanfattning : The serendipitous discovery of the potent cytotoxic properties of cisplatin brought about a revolution in the treatment of certain types of cancer, but almost fifty years later, there still remain unknown areas in the chemistry of cisplatin. There are questions regarding which form of the drug reaches its DNA target, or why certain DNA sequences are more preferred than others for reaction with cisplatin. LÄS MER

  3. 3. Refined in vitro Models for Prediction of Intestinal Drug Transport : Role of pH and Extracellular Additives in the Caco-2 Cell Model

    Författare :Sibylle Neuhoff; Per Artursson; Anna-Lena Ungell; Patrick Augustijns; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmacy; Caco-2 cells; membrane permeability; drug permeation; drug efflux ratios; drug uptake ratios; Cremophor EL; bovine serum albumin; pH-dependent permeability; drug transport; FARMACI; PHARMACY; FARMACI;

    Sammanfattning : Drug transport across the intestinal epithelium is roughly predicted from permeability values obtained from Caco-2 cell monolayers. This thesis examines the important role of pH and extracellular additives for increasing the reliability and predictivity of the in vitro screening system, Caco-2. LÄS MER

  4. 4. Fragment-based drug discovery : Novel methods and strategies for identifying and evolving fragment leads

    Författare :Edward A. FitzGerald; Helena Danielson; Hanna-Kirsti Schrøder Leiros; Uppsala universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; Drug Discovery; Biophysics; Fragment-based drug discovery; Epigenetics; Biosensors; Surface Plasmon Resonance; Interaction Analysis; Second-Harmonics; Biokemi; Biochemistry;

    Sammanfattning : The need for new drugs became ever more apparent in the year 2020 when the world was faced with a viral pandemic. How drugs are discovered and their relevance to society became part of daily discussions in workplaces and homes throughout the world. Consequently, efficient strategies for preclinical drug discovery are clearly needed. LÄS MER

  5. 5. Kinetic studies of NS3 and NS5B from Hepatitis C virus : Implications and applications for drug discovery

    Författare :Göran Dahl; Helena Danielson; Raffaele De Francesco; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Hepatitis C virus; NS3; NS5B; enzyme kinetics; inhibition; resistance; drug; Biochemistry; Biokemi; Biokemi; Biochemistry;

    Sammanfattning : The aim of these studies was to increase our understanding of the non-structural proteins 3 and 5B (NS3 and NS5B) from the hepatitis C virus (HCV), and thereby contribute to the development of new and better drugs against HCV.By studying NS3 with substitutions identified to be associated with resistance to NS3 inhibitors in clinical trials (R155Q, A156T and D168V) it was found that not all inhibitors were affected, indicating that cross-resistance can be avoided. LÄS MER