Bile Acids, Nuclear Receptors and Cytochrome P450
| Autor: | Ondřej Zendulka, Jan Juřica, Kristýna Nosková, Gabriela Přibyl Dovrtělová |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Physiology Receptors Cytoplasmic and Nuclear Calcitriol receptor Xenobiotics Bile Acids and Salts 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Cytochrome P-450 Enzyme System Animals Humans Receptor chemistry.chemical_classification Pregnane X receptor biology Cytochrome P450 General Medicine Metabolism 3. Good health 030104 developmental biology Enzyme Liver chemistry Biochemistry Nuclear receptor biology.protein 030211 gastroenterology & hepatology Xenobiotic |
| Zdroj: | ResearcherID Scopus-Elsevier |
| ISSN: | 1802-9973 0862-8408 |
| Popis: | This review summarizes the importance of bile acids (BA) as important regulators of various homeostatic mechanisms with detailed focus on cytochrome P450 (CYP) enzymes. In the first part, synthesis, metabolism and circulation of BA is summarized and BA are reviewed as physiological ligands of nuclear receptors which regulate transcription of genes involved in their metabolism, transport and excretion. Notably, PXR, FXR and VDR are the most important nuclear receptors through which BA regulate transcription of CYP genes involved in the metabolism of both BA and xenobiotics. Therapeutic use of BA and their derivatives is also briefly reviewed. The physiological role of BA interaction with nuclear receptors is basically to decrease production of toxic non-polar BA and increase their metabolic turnover towards polar BA and thus decrease their toxicity. By this, the activity of some drug-metabolizing CYPs is also influenced what could have clinically relevant consequences in cholestatic diseases or during the treatment with BA or their derivatives. |
| Databáze: | OpenAIRE |
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