Prague Med. Rep. 2013, 114, 205-213

Pregnane Xenobiotic Receptors and Their Effect on Drug Elimination from the Organism

Martin Šíma*, I. Netíková, O. Slanař

Institute of Pharmacology, First Faculty of Medicine, Charles University in Prague and General University Hospital in Prague, Prague, Czech Republic

Nuclear receptors are intracellular proteins which, having been activated by their more or less specific ligands, regulate (usually increase) the transcription of target genes. They thus participate in a regulation of a number of physiologic functions. Some of them – especially pregnane xenobiotic receptors – serve primarily as protection of the organism from the xenobiotic intoxication. This is because many xenobiotics activate their function which consists in increasing the gene expression of enzymes involved in the metabolism of xenobiotics and detoxication drug transporters. Clarification of these mechanisms enabled the understanding of the substance of many drug-drug interactions observed in the clinical practice. Polymorphism of the nuclear receptors appears to be one of the causes of the interindividual variability in response to drug administration.


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