Biology:SLC10A2
Generic protein structure example |
The SLC10A2 (solute carrier family 10 member 2) gene in humans encodes the bile acid:sodium symporter known as the apical sodium–bile acid transporter (ASBT) or as the ileal bile acid transporter (IBAT).[1][2]
ASBT/IBAT is most highly expressed in the ileum, where it is found on the brush border membrane of enterocytes. It is responsible for the initial uptake of bile acids, particularly conjugated bile acids, from the intestine as part of their enterohepatic circulation.[3]
As a drug target
Several medications to inhibit IBAT are under development. They include elobixibat, under development for the treatment of constipation and irritable bowel syndrome,[4] and volixibat, under development for the treatment of nonalcoholic steatohepatitis.[5]
See also
References
- ↑ "Localization of the ileal sodium-bile acid cotransporter gene (SLC10A2) to human chromosome 13q33". Genomics 33 (3): 538–40. May 1996. doi:10.1006/geno.1996.0233. PMID 8661017.
- ↑ "Entrez Gene: SLC10A2 solute carrier family 10 (sodium/bile acid cotransporter family), member 2". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6555.
- ↑ "Role of the intestinal bile acid transporters in bile acid and drug disposition". Handbook of Experimental Pharmacology (201): 169–203. 2011. doi:10.1007/978-3-642-14541-4_4. PMID 21103970.
- ↑ "Elobixibat and its potential role in chronic idiopathic constipation". Therapeutic Advances in Gastroenterology 7 (4): 167–75. July 2014. doi:10.1177/1756283X14528269. PMID 25057297.
- ↑ Chitnis, Deepak (2016-08-03), [tt_news=529065&cHash=0318868cbd3098688c489deca5797e62 "FDA grants fast track status to volixibat"], Internal Medicine News Digital Network, http://www.internalmedicinenews.com/index.php?id=514&tx_ttnews[tt_news]=529065&cHash=0318868cbd3098688c489deca5797e62, retrieved 2016-08-14.
Further reading
- "Intestinal bile acid transport: biology, physiology, and pathophysiology". Journal of Pediatric Gastroenterology and Nutrition 32 (4): 407–17. April 2001. doi:10.1097/00005176-200104000-00002. PMID 11396803.
- "Apical sodium dependent bile acid transporter (ASBT, SLC10A2): a potential prodrug target". Molecular Pharmaceutics 3 (3): 223–30. 2006. doi:10.1021/mp060022d. PMID 16749855.
- "Identification of a mutation in the ileal sodium-dependent bile acid transporter gene that abolishes transport activity". The Journal of Biological Chemistry 270 (45): 27228–34. November 1995. doi:10.1074/jbc.270.45.27228. PMID 7592981.
- "Primary bile acid malabsorption caused by mutations in the ileal sodium-dependent bile acid transporter gene (SLC10A2)". The Journal of Clinical Investigation 99 (8): 1880–7. April 1997. doi:10.1172/JCI119355. PMID 9109432.
- "Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter". The American Journal of Physiology 274 (1 Pt 1): G157-69. January 1998. PMID 9458785.
- "Absence of dysfunctional ileal sodium-bile acid cotransporter gene mutations in patients with adult-onset idiopathic bile acid malabsorption". Scandinavian Journal of Gastroenterology 36 (10): 1077–80. October 2001. doi:10.1080/003655201750422693. PMID 11589382.
- "Analysis of the ileal bile acid transporter gene, SLC10A2, in subjects with familial hypertriglyceridemia". Arteriosclerosis, Thrombosis, and Vascular Biology 21 (12): 2039–45. December 2001. doi:10.1161/hq1201.100262. PMID 11742882.
- "Human apical sodium-dependent bile salt transporter gene (SLC10A2) is regulated by the peroxisome proliferator-activated receptor alpha". The Journal of Biological Chemistry 277 (34): 30559–66. August 2002. doi:10.1074/jbc.M203511200. PMID 12055195.
- "Transport of bile acids in multidrug-resistance-protein 3-overexpressing cells co-transfected with the ileal Na+-dependent bile-acid transporter". The Biochemical Journal 369 (Pt 1): 23–30. January 2003. doi:10.1042/BJ20021081. PMID 12220224.
- "Genetic and physiological data implicating the new human gene G72 and the gene for D-amino acid oxidase in schizophrenia". Proceedings of the National Academy of Sciences of the United States of America 99 (21): 13675–80. October 2002. doi:10.1073/pnas.182412499. PMID 12364586.
- "Bile acid-induced negative feedback regulation of the human ileal bile acid transporter". Hepatology 40 (1): 149–56. July 2004. doi:10.1002/hep.20295. PMID 15239098.
- "Degradation of the apical sodium-dependent bile acid transporter by the ubiquitin-proteasome pathway in cholangiocytes". The Journal of Biological Chemistry 279 (43): 44931–7. October 2004. doi:10.1074/jbc.M400969200. PMID 15304498.
- "Topology scanning and putative three-dimensional structure of the extracellular binding domains of the apical sodium-dependent bile acid transporter (SLC10A2)". Biochemistry 43 (36): 11380–92. September 2004. doi:10.1021/bi049270a. PMID 15350125.
- "Site-directed mutagenesis and use of bile acid-MTS conjugates to probe the role of cysteines in the human apical sodium-dependent bile acid transporter (SLC10A2)". Biochemistry 44 (24): 8908–17. June 2005. doi:10.1021/bi050553s. PMID 15952798.
- "Ileal bile acid-binding protein, functionally associated with the farnesoid X receptor or the ileal bile acid transporter, regulates bile acid activity in the small intestine". The Journal of Biological Chemistry 280 (51): 42283–9. December 2005. doi:10.1074/jbc.M507454200. PMID 16230354.
- "Apical sodium bile acid transporter and ileal lipid binding protein in gallstone carriers". Journal of Lipid Research 47 (1): 42–50. January 2006. doi:10.1194/jlr.M500215-JLR200. PMID 16237211.
- "Membrane topology of human ASBT (SLC10A2) determined by dual label epitope insertion scanning mutagenesis. New evidence for seven transmembrane domains". Biochemistry 45 (3): 943–53. January 2006. doi:10.1021/bi052202j. PMID 16411770.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.