bile acid receptor; nuclear receptor subfamily 1 group H member 4; farnesoid X-activated receptor; farnesol receptor HRR-1; retinoid X receptor-interacting protein 14; RXR-interacting protein 14 (NR1H4, BAR, FXR, HRR1, RIP14)
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Function
- receptor for bile acids
- transcriptional repression of CYP7A1 gene
- activates intestinal bile acid-binding protein (IBABP)
- bile acid/FXR complex forms nuclear heterodimer with RXR
- interacts with CARM1 & SMARD1
- upregulates expression of ACE2 (receptor for SARS-Cov2)[8]
Structure
- belongs to the nuclear hormone receptor family, NR1 subfamily
- contains 1 nuclear receptor DNA-binding domain
Compartment
- cytoplasm, nucleus
- binds to bile acid in the cytoplasm
- the bile acid/FXR receptor complex migrates into the cell nucleus
Alternative splicing
named isoforms=4
Pharmacology
- binds to & is inhibited by ursodiol
- upregulates ACE2 (receptor for SARS Cov2) in lung & intestine
- inhibition by ursodiol may inhibit Covid-19 infection[8]
Comparative biology
- in mice, binding of bile acids to the nuclear receptor FXR plays a role in benefits of vertical sleeve gastrectomy[3]
- higher levels of circulating bile acids
More general terms
References
- ↑ UniProt http://www.uniprot.org/uniprot/Q96RI1.html
- ↑ Wikipedia; farnesoid X receptor entry http://en.wikipedia.org/wiki/farnesoid_X_receptor
- ↑ 3.0 3.1 Ryan KK et al. FXR is a molecular target for the effects of vertical sleeve gastrectomy. Nature 2014 May 8; 509:183 PMID: https://www.ncbi.nlm.nih.gov/pubmed/24670636
- ↑ Wang H, Chen J, Hollister K, Sowers LC, Forman BM Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. Mol Cell. 1999 May;3(5):543-53. PMID: https://www.ncbi.nlm.nih.gov/pubmed/10360171
- ↑ Claudel T, Sturm E, Kuipers F, Staels B The farnesoid X receptor: a novel drug target? Expert Opin Investig Drugs. 2004 Sep;13(9):1135-48. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15330745
- ↑ Downes M, Verdecia MA, Roecker AJ et al A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol Cell. 2003 Apr;11(4):1079-92 PMID: https://www.ncbi.nlm.nih.gov/pubmed/12718892
- ↑ Biocarta: FXR and LXR Regulation of Cholesterol Metabolism http://www.biocarta.com/pathfiles/m_fxrpathway.asp
- ↑ 8.0 8.1 8.2 Brevini T, Maes M, Webb GJ et al FXR inhibition may protect from SARS-CoV-2 infection by reducing ACE2. Nature 2022. Dec 5. PMID: https://www.ncbi.nlm.nih.gov/pubmed/36470304 https://www.nature.com/articles/s41586-022-05594-0