Target Information

Target General Infomation
Target ID
T24982
Former ID
TTDNC00442
Target Name
Ileal bile acid transfer
Gene Name
SLC10A2
Synonyms
ASBT; Apical sodiumdependent bile acid transporter; IBAT; ISBT; Ileal Na(+)/bile acid cotransporter; Ileal sodium/bile acid cotransporter; Ileal sodiumdependent bile acid transporter; Na(+)dependent ileal bile acid transporter; Sodium/taurocholate cotransporting polypeptide, ileal; Solute carrier family 10 member 2; SLC10A2
Target Type
Clinical Trial
Disease Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Lipid metabolism disorder [ICD10: E75-E78]
Primary biliary cirrhosis [ICD9: 571.6; ICD10: K74.3]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Unspecified [ICD code not available]
Function
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
BioChemical Class
Bile acid:na(+) symporter
UniProt ID
Q12908
Sequence
MNDPNSCVDNATVCSGASCVVPESNFNNILSVVLSTVLTILLALVMFSMGCNVEIKKFLG
HIKRPWGICVGFLCQFGIMPLTGFILSVAFDILPLQAVVVLIIGCCPGGTASNILAYWVD
GDMDLSVSMTTCSTLLALGMMPLCLLIYTKMWVDSGSIVIPYDNIGTSLVSLVVPVSIGM
FVNHKWPQKAKIILKIGSIAGAILIVLIAVVGGILYQSAWIIAPKLWIIGTIFPVAGYSL
GFLLARIAGLPWYRCRTVAFETGMQNTQLCSTIVQLSFTPEELNVVFTFPLIYSIFQLAF
AAIFLGFYVAYKKCHGKNKAEIPESKENGTEPESSFYKANGGFQPDEK
Drugs and Mode of Action
Drug(s) A-3309 Drug Info Phase 3 Lipid metabolism disorder [524353]
264W94 Drug Info Phase 2 Hyperlipidaemia [531629], [541657]
GSK2330672 Drug Info Phase 2 Type 2 diabetes [532355]
LUM001 Drug Info Phase 2 Primary biliary cirrhosis [525031]
S-8921 Drug Info Phase 2 Hyperlipidaemia [534690]
1614235 + 2330672 Drug Info Phase 1 Type 2 diabetes [549464]
Modulator 1614235 + 2330672 Drug Info [543982]
264W94 Drug Info [531629]
AZD-7806 Drug Info [532143]
GSK2330672 Drug Info [532355]
[3H]taurocholic acid Drug Info [534551]
Inhibitor A-3309 Drug Info [532143]
LUM001 Drug Info [550354]
S-8921 Drug Info [534690]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Bile secretion
Reactome Recycling of bile acids and salts
WikiPathways Bile acid and bile salt metabolism
References
Ref 524353ClinicalTrials.gov (NCT01895543) Safety and Tolerability Extension Trial for Patients With Chronic Idiopathic Constipation. U.S. National Institutes of Health.
Ref 525031ClinicalTrials.gov (NCT02321306) An Open-label Study to Evaluate the Long-term Safety and Tolerability of LUM001 in Patients With Primary Biliary Cirrhosis. U.S. National Institutes of Health.
Ref 531629Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes. Am J Physiol Endocrinol Metab. 2012 Jan 1;302(1):E68-76.
Ref 532355Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114.
Ref 534690Inhibition of ileal Na+/bile acid cotransporter by S-8921 reduces serum cholesterol and prevents atherosclerosis in rabbits. Arterioscler Thromb Vasc Biol. 1998 Aug;18(8):1304-11.
Ref 541657(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6529).
Ref 549464Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037723)
Ref 531629Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes. Am J Physiol Endocrinol Metab. 2012 Jan 1;302(1):E68-76.
Ref 532143Elobixibat for the treatment of constipation. Expert Opin Investig Drugs. 2013 Feb;22(2):277-84.
Ref 532355Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114.
Ref 534551Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter. Am J Physiol. 1998 Jan;274(1 Pt 1):G157-69.
Ref 534690Inhibition of ileal Na+/bile acid cotransporter by S-8921 reduces serum cholesterol and prevents atherosclerosis in rabbits. Arterioscler Thromb Vasc Biol. 1998 Aug;18(8):1304-11.
Ref 543982(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 960).
Ref 550354Current research on the treatment of primary sclerosing cholangitis. Intractable Rare Dis Res. 2015 Feb; 4(1): 1-6.

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