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1. 21. Metabolism of quinoline 3-carboxamide compounds, a group of synthetic immunomodulators, in various species

   Författare :Helen Tuvesson; Institutionen för experimentell medicinsk vetenskap; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; enzymologi; Proteiner; enzymology; Proteins; Gastroenterologi; Gastro-enterology; pharmacokinetics; enzyme kinetics; quinoline 3-carboxamides; Keywords: Metabolism; cytochrome P450;

   Sammanfattning : Cytochrome P450 (CYP) is involved in the metabolism of the majority of clinically used drugs. We have studied the CYP mediated metabolism of quinoline 3-carboxamides, a group of synthetic immunomodulators in liver microsomal preparations from various species. LÄS MER

3. 22. Novel Fatty Acid Dioxygenases of Human and Plant Pathogenic Fungi : Studies by Gene Deletion and Expression

   Författare :Fredrik Jernerén; Ernst Oliw; Ivo Feussner; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; aspergilli; dioxygenase; oxygenase; Magnaporthe oryzae; Gaeumannomyces graminis; Lasiodiplodia theobromae; jasmonic acid; linoleate diol synthase; cyclooxygenase; prostaglandin H synthase; cytochrome P450; oxylipin; hydroperoxide isomerase; allene oxide synthase; Pharmaceutical pharmacology; Farmaceutisk farmakologi; Biochemical Pharmacology; Biokemisk farmakologi;

   Sammanfattning : The dioxygenase-cytochrome P450 fusion proteins (DOX-CYP) comprise a heme-containing enzyme family that shares structural and catalytic properties with mammalian prostaglandin H (PGH) synthases. 7,8-Linoleate diol synthase (7,8-LDS) of Gaeumannomyces graminis was first characterized, and DOX-CYP enzymes are of mechanistic and biological interest. LÄS MER

4. 23. Catalytic and Structural Properties of Heme-containing Fatty Acid Dioxygenases : Similarities of Fungal Dioxygenases and Cyclooxygenases

   Författare :Ulrike Garscha; Ernst Oliw; Per-Johan Jakobsson; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; dioxygenase; prostaglandin H synthase; Gaeumannomyces graminis; Aspergilli; hydroperoxide isomerase; linoleate diol synthase; cytochrome P450; oxylipin; Pharmaceutical pharmacology; Farmaceutisk farmakologi; Farmaceutisk farmakologi; Pharmaceutical Pharmacology;

   Sammanfattning : 7,8-Linoleate diol synthase (7,8-LDS) of the take-all pathogen of wheat, Gaeumannomyces graminis, converts linoleic acid to 8R-hydroperoxyoctadecadienoic acid (8-HPODE) by 8-dioxygenase activity (8-DOX), and further isomerizes the hydroperoxide to 7S,8S-dihydroxyoctadecadienoic acid (7,8-DiHODE) by hydroperoxide isomerase activity. Sequence alignment showed homology to prostaglandin H synthase (PGHS), and both enzymes share structural and catalytic properties. LÄS MER

5. 24. Modeling the Interaction Space of Biological Macromolecules: A Proteochemometric Approach : Applications for Drug Discovery and Development

   Författare :Aleksejs Kontijevskis; Jarl Wikberg; Jan Komorowski; Robert Glen; Uppsala universitet; []
   Nyckelord :Bioinformatics; proteochemometrics; bioinformatics; chemoinformatics; chemical space; QSAR; retroviral proteases; HIV-1; drug resistance; pharmacogenomics; cytochrome P450; GPCRs; melanocortin receptors; interactome; machine-learning; rough sets; Bioinformatik;

   Sammanfattning : Molecular interactions lie at the heart of myriad biological processes. Knowledge of molecular recognition processes and the ability to model and predict interactions of any biological molecule to any chemical compound are the key for better understanding of cell functions and discovery of more efficacious medicines. LÄS MER

7. 25. Growth hormone regulation of hepatic drug-metabolising enzymes in humans and rats

   Författare :Eva Rasmussen; Uppsala universitet; []
   Nyckelord :Medical sciences; growth hormone; IGF-I; somatostatin; cytochrome P450; regulation; MEDICIN OCH VÅRD; MEDICINE; MEDICIN; klinisk farmakologi; Clinical Pharmacology;

   Sammanfattning : There are pronounced sex-differences in the gene expression of several liver enzymes in the rat. The sex-differentiated secretion of growth hormone (GH) regulates these differences. We wanted to further investigate the mechanisms of this regulation in rats and to study the GH regulation of drug metabolism in man. LÄS MER