It is part of the superfamily of nuclear receptors. FXR is expressed in the liver and ileum. The gene encoding this protein is localized on human chromosome 12q23.1.[1]
Biochem./physiol. Wirkung
Farnesoid-X-activated receptor (FXR) was originally identified and cloned in rat as an orphan nuclear hormone receptor based on hybridization with a degenerate oligonucleotide designed from the highly conserved nuclear hormone receptor DNA binding domain. FXR functions as a heterodimer with RXR and binds to sequence elements in the promoters of target genes. The FXR/RXR heterodimer binds with highest affinity to inverted repeats separated by 1 bp (IR-1) and with low affinity to direct repeats separated by 4 and 5 bp (DR-4 and DR-5). As is the case for other nuclear hormone receptors, FXR regulates target gene activity in response to ligand. While initial studies suggested that farnesol and retinoid metabolites were likely ligands for FXR, current data support the notion that FXR is a bile acid sensor that plays an integral role in bile acid synthesis and transport. In the small intestine, FXR regulates bile acid uptake through the upregulation of the ileal bile acid binding protein gene via binding to an upstream response element. The FXR/RXR heterodimer can be activated by the bile salt chenodeoxycholic acid (CDCA) and FXR is required for the bile salt-dependent transcriptional control of the human ABCB11 gene (the bile salt export pump). In addition, FXR has been shown to inhibit the cholesterol 7-hydrolase gene (CYP7A1) transcription.
Physikalische Form
Clear and colorless frozen liquid solution
Angaben zur Herstellung
Use a manual defrost freezer and avoid repeated freeze-thaw cycles. While working, please keep sample on ice.
Farnesoid X Receptor and Bile Salts Are Involved in
Transcriptional Regulation of the Gene Encoding
the Human Bile Salt Export Pump
Jacqueline R.M. Plass
Hepatology (2001)
Farnesoid X Receptor (FXR) Activation and FXR Genetic Variation in Inflammatory Bowel Disease
Rian M. Nijmeijer
PLoS ONE, 6(8), e23745-e23745 (2011)
Down-regulation of Cholesterol 7a-Hydroxylase (CYP7A1) Gene Expression by Bile Acids in Primary Rat Hepatocytes Is Mediated by the c-Jun N-terminal Kinase Pathway*
Seema Gupta
The Journal of Biological Chemistry, 276 (2001)
General molecular biology and architecture of nuclear receptors.
Pawlak M et al
Current Topics in Medicinal Chemistry, 12(6), 486-504 (2012)
Proceedings of the National Academy of Sciences of the United States of America, 94(15), 7909-7914 (1997-07-22)
Retinoids are crucial regulators of a wide variety of processes in both developing and adult animals. These effects are thought to be mediated by the retinoic acid (RA) receptors and the retinoid X receptors (RXRs). We have identified an additional
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