Farnesoid X Receptor Agonist Represses Cytochrome P450 2D6 Expression by Upregulating Small Heterodimer Partner.

Title

Farnesoid X Receptor Agonist Represses Cytochrome P450 2D6 Expression by Upregulating Small Heterodimer Partner.

Creator

Pan Xian; Lee Yoon-Kwang; Jeong Hyunyoung

Publisher

Drug metabolism and disposition: the biological fate of chemicals

Date

2015
2015-07

Description

Cytochrome P450 2D6 (CYP2D6) is a major drug-metabolizing enzyme responsible for eliminating approximately 20% of marketed drugs. Studies have shown that differential transcriptional regulation of CYP2D6 may contribute to large interindividual variability in CYP2D6-mediated drug metabolism. However, the factors governing CYP2D6 transcription are largely unknown. We previously demonstrated small heterodimer partner (SHP) as a novel transcriptional repressor of CYP2D6 expression. SHP is a representative target gene of the farnesoid X receptor (FXR). The objective of this study is to investigate whether an agonist of FXR,

Subject

Animals; Cytochrome P-450 CYP2D6/*biosynthesis; Cytochrome P-450 Enzyme Inhibitors/*pharmacology; Cytoplasmic and Nuclear/*agonists; Enzymologic/drug effects; Gene Expression Regulation; Genetic/drug effects/genetics; HEK293 Cells; Hepatocytes/drug effects/enzymology/metabolism; Humans; Isoxazoles/*pharmacology; Knockout; Mice; Receptors; Transcription; Transgenic

Rights

Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).

Pages

1002–1007

Issue

7

Volume

43

Citation

Pan Xian; Lee Yoon-Kwang; Jeong Hyunyoung, “Farnesoid X Receptor Agonist Represses Cytochrome P450 2D6 Expression by Upregulating Small Heterodimer Partner.,” NEOMED Bibliography Database, accessed December 6, 2021, https://neomed.omeka.net/items/show/4521.

Social Bookmarking