Advanced Course on Xenobiotic Metabolism
1. Eleni Rekka - Introduction: Purpose of xenobiotic metabolism in the organism. Organs and xenobiotic metabolising enzyme systems of the organism. Phases of xenobiotic metabolism (I, II and III). Biointoxication, biodetoxication. –Cytochrome P450 enzyme superfamily: Structure, binding, type I, II and reverse type II spectra, Catalytic circle, Evolution, division and catalytic activity. Induction and inhibition. Relation with peroxisomes. Cytochrome P450 enzymes in the metabolism of xenobiotics. –Non cytochrome P450 enzymes in the metabolism of xenobiotics: Carboxyesterases, Glutathione-S-transferases, Epoxide hydrolases. –Drug design based on xenobiotic metabolism. 2. Panagiotis Kourounakis -Xenobiotic oxidations by the flavin containing monoxygenases (FMO): Structure, characteristics, substrates, inducers, examples. –Aminoxidases and drug metabolism: Structure, specificity, distribution in the organism, regulation and turnover. Xenobiotic primary amines. Metabolism of xenobiotics via primary amines. Inhibition by acetylenic compounds and mechanism. –Prodrugs, chemical delivery systems. –Stress and xenobiotic metabolism. –Brain and xenobiotic metabolism.