Search for dissertations about: "drug discovery"

Showing result 6 - 10 of 286 swedish dissertations containing the words drug discovery.

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

   Author : Andrea Treyer; Per Artursson; Gert Fricker; Uppsala universitet; []
   Keywords : 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

4. 7. Protease Activity, Inhibition and Ligand Interaction Analysis : Developments and Applications for Drug Discovery

   Author : Thomas Gossas; Helena Danielson; Mikael Widersten; Alexander Wlodawer; Uppsala universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; proteases; kinetics; biosensors; inhibition; calcium; drug discovery; Biokemi;

   Abstract : The present study has focused on characterising protease-ligand interactions in the context of drug discovery. The proteases that have been studied are human matrix metallopeptidase 12 (MMP-12), HIV-protease and Hepatitis C virus (HCV) NS3/NS4A protease. READ MORE

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

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

   Abstract : 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. READ MORE

6. 9. Analysis of the interaction between HIV-1 protease and inhibitors : Applications for drug discovery

   Author : Per-Olof Markgren; Uppsala universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; Biokemi; Biochemistry; Biokemi; Biokemi; Biochemistry;

   Abstract : The aims of this study were to identify and characterize inhibitors of HIV-l protease aspotential leads in a drug discovery process, and to develop improved methods for suchcharacterization. More than 300 inhibitors, including linear and cyclic peptidomimetictransition state analogs and Cu2+, were analyzed. READ MORE

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

   Author : Maria T. Lindgren; Helena Danielson; Jozsef Tözser; Uppsala universitet; []
   Keywords : 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