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Lecturer(s)
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Dvořák Zdeněk, prof. RNDr. DrSc.
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Course content
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Xenobiotics, metabolism of xenobiotics, three phases of biotransformation. Phase I of biotransformation - hydrolytic and red-ox reactions; cytochrome P450 (CYP)-dependent microsomal monooxygenases; nomenclature and function of CYP; flavine microsomal monooxygenases; alcohol- and aldehyde-dehydrogenases. Phase II of biotransformation - conjugation reactions; glucuronidation, sulfatation; conjugation with amino acids, glutathione; methylation and acetylation; rhodanase. Phase III of biotransformation - cellular transport systems for xenobiotics; P-glycoprotein, MRP transporting protein (multidrug resistance associated protein); OATP, OCTP. Regulation of biotransformation enzymes - factors affecting activity of biotransformation enzymes; enzyme induction (phenobarbital, dioxin); aryl hydrocarbon receptor AhR, role and function of receptors PXR, CAR, GR, RXR, VDR; enzyme inhibition; drug interactions.
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Learning activities and teaching methods
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Dialogic Lecture (Discussion, Dialog, Brainstorming)
- Preparation for the Exam
- 50 hours per semester
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Learning outcomes
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Xenobiotics, metabolism of xenobiotics, three phases of biotransformation. Phase I of biotransformation - hydrolytic and red-ox reactions; cytochrome P450 (CYP)-dependent microsomal monooxygenases; nomenclature and function of CYP; flavine microsomal monooxygenases; alcohol- and aldehyde-dehydrogenases. Phase II of biotransformation - conjugation reactions; glucuronidation, sulfatation; conjugation with amino acids, glutathione; methylation and acetylation; rhodanase. Phase III of biotransformation - cellular transport systems for xenobiotics; P-glycoprotein, MRP transporting protein (multidrug resistance associated protein); OATP, OCTP. Regulation of biotransformation enzymes - factors affecting activity of biotransformation enzymes; enzyme induction (phenobarbital, dioxin); aryl hydrocarbon receptor AhR, role and function of receptors PXR, CAR, GR, RXR, VDR; enzyme inhibition; drug interactions.
Explain main aspects of the xenobiochemistry, generalize pathways of the distribution and the biotransformation of xenobiotics.
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Prerequisites
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Biochemistry knowledge.
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Assessment methods and criteria
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Oral exam
The candidate is expected to conduct scientific discussion in broader context of the whole discipline.
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Recommended literature
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Kvasničková E. (1998). Xenobiochemie. FaF UK Praha.
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