Target Information

Target General Infomation
Target ID
T24982 (Former ID: TTDNC00442)
Target Name
Ileal sodium/bile acid cotransporter (SLC10A2)
Synonyms
Solute carrier family 10 member 2; Sodium/taurocholate cotransporting polypeptide, ileal; SLC10A2; Na(+)dependent ileal bile acid transporter; Ileal sodiumdependent bile acid transporter; Ileal Na(+)/bile acid cotransporter; ISBT; IBAT; Apical sodiumdependent bile acid transporter; ASBT
Gene Name
SLC10A2
Target Type
Clinical trial target
 [1]
Disease [+] 1 Target-related Diseases +
1 Inborn lipid metabolism error [ICD-11: 5C52]
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.
UniProt ID
NTCP2_HUMAN
Sequence
MNDPNSCVDNATVCSGASCVVPESNFNNILSVVLSTVLTILLALVMFSMGCNVEIKKFLG
HIKRPWGICVGFLCQFGIMPLTGFILSVAFDILPLQAVVVLIIGCCPGGTASNILAYWVD
GDMDLSVSMTTCSTLLALGMMPLCLLIYTKMWVDSGSIVIPYDNIGTSLVSLVVPVSIGM
FVNHKWPQKAKIILKIGSIAGAILIVLIAVVGGILYQSAWIIAPKLWIIGTIFPVAGYSL
GFLLARIAGLPWYRCRTVAFETGMQNTQLCSTIVQLSFTPEELNVVFTFPLIYSIFQLAF
AAIFLGFYVAYKKCHGKNKAEIPESKENGTEPESSFYKANGGFQPDEK
Drugs and Modes of Action
Clinical Trial Drug(s) [+] 7 Clinical Trial Drugs +
1 A-3309 Drug Info Phase 3 Lipid metabolism disorder [2]
2 264W94 Drug Info Phase 2 Hyperlipidaemia [3], [4]
3 GSK2330672 Drug Info Phase 2 Type-2 diabetes [5]
4 LUM001 Drug Info Phase 2 Primary biliary cirrhosis [6]
5 S-8921 Drug Info Phase 2 Hyperlipidaemia [7]
6 Taurocholic Acid Drug Info Phase 1/2 Type-2 diabetes [8]
7 1614235 + 2330672 Drug Info Phase 1 Type-2 diabetes [9]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 3 Inhibitor drugs +
1 A-3309 Drug Info [1]
2 LUM001 Drug Info [10]
3 S-8921 Drug Info [7]
Modulator [+] 5 Modulator drugs +
1 264W94 Drug Info [4]
2 GSK2330672 Drug Info [5]
3 Taurocholic Acid Drug Info [11]
4 1614235 + 2330672 Drug Info [12]
5 AZD-7806 Drug Info [1]
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Expression Profile Info 
Target Affiliated Biological Pathways
KEGG Pathway [+] 1 KEGG Pathways +
1 Bile secretion
Reactome [+] 1 Reactome Pathways +
1 Recycling of bile acids and salts
WikiPathways [+] 1 WikiPathways +
1 Bile acid and bile salt metabolism
References
REF 1 Elobixibat for the treatment of constipation. Expert Opin Investig Drugs. 2013 Feb;22(2):277-84.
REF 2 ClinicalTrials.gov (NCT01895543) Safety and Tolerability Extension Trial for Patients With Chronic Idiopathic Constipation. U.S. National Institutes of Health.
REF 3 URL: 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 4 Inhibition 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 5 Discovery 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 6 ClinicalTrials.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 7 Inhibition 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 8 URL: 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: 4547).
REF 9 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037723)
REF 10 Current research on the treatment of primary sclerosing cholangitis. Intractable Rare Dis Res. 2015 Feb; 4(1): 1-6.
REF 11 Expression 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 12 URL: 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).

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