The nuclear orphan protein bile acid receptor aka farnesoid ...

created [InstanceEdit:5340205] Jassal, Bijay, 2014-03-12
dbId 5340176
displayName The nuclear orphan protein bile acid receptor aka farnesoid ...
modified [InstanceEdit:5340257] Jassal, Bijay, 2014-03-13
schemaClass Summation
text The nuclear orphan protein bile acid receptor aka farnesoid X-activated receptor (NR1H4 aka FXR) can be activated by bile acids and their salts, its physiological ligands. Mouse Nrih4 is highly expressed in the liver, intestine, kidney and adrenal gland, and to a lesser extent in white adipose tissue and heart (Zhang et al. 2003). Bile acids tested to activate NR1H4 are chenodeoxycholic acid (CDCA), lithocholic acid (LCHA) and deoxycholic acid (DCA) (Parks et al. 1999, Makishima et al. 1999).

Once bound to its ligand, activated NR1H4 binds to retinoic acid receptor RXR-alpha (RXRA) and either nuclear receptor coactivator 1 or 2 (NCOA1 or 2) to function as a ligand-activated transcription factor. This complex repressed transcription of the CYP7A1 gene (encoding cholesterol 7alpha-hydroxylase, the rate-limiting enzyme in bile acid synthesis) (Holt et al. 2003) and activated the SLC10A2 and 6 genes (encoding Ileal sodium/bile acid cotransporters, both bile acid transporters) (Plass et al. 2002, Ananthanarayanan et al. 2001). Thus, NR1H4 is one of the most important regulators of bile acid metabolism, regulating bile acid synthesis, conjugation, secretion and uptake (Lee et al. 2006, Houten et al. 2006).
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