|
Lecturer(s)
|
-
Dvořák Zdeněk, prof. RNDr. DrSc.
-
Šebela Marek, prof. Mgr. Dr.
|
|
Course content
|
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.
|
|
Learning activities and teaching methods
|
Dialogic Lecture (Discussion, Dialog, Brainstorming)
- Preparation for the Exam
- 50 hours per semester
|
|
Learning outcomes
|
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.
|
|
Prerequisites
|
Biochemistry knowledge.
|
|
Assessment methods and criteria
|
Oral exam
The candidate is expected to conduct scientific discussion in broader context of the whole discipline.
|
|
Recommended literature
|
-
Kvasničková E. (1998). Xenobiochemie. FaF UK Praha.
-
Skálová L. a kol. Metabolismus léčiv a jiných xenobiotik 978-80-2463-733-4.
|