Target Information
Target General Infomation | |||||
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Target ID |
T24982
(Former ID: TTDNC00442)
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Target Name |
Ileal sodium/bile acid cotransporter (SLC10A2)
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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
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Gene Name |
SLC10A2
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Target Type |
Clinical trial target
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[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.
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UniProt ID | |||||
Sequence |
MNDPNSCVDNATVCSGASCVVPESNFNNILSVVLSTVLTILLALVMFSMGCNVEIKKFLG
HIKRPWGICVGFLCQFGIMPLTGFILSVAFDILPLQAVVVLIIGCCPGGTASNILAYWVD GDMDLSVSMTTCSTLLALGMMPLCLLIYTKMWVDSGSIVIPYDNIGTSLVSLVVPVSIGM FVNHKWPQKAKIILKIGSIAGAILIVLIAVVGGILYQSAWIIAPKLWIIGTIFPVAGYSL GFLLARIAGLPWYRCRTVAFETGMQNTQLCSTIVQLSFTPEELNVVFTFPLIYSIFQLAF AAIFLGFYVAYKKCHGKNKAEIPESKENGTEPESSFYKANGGFQPDEK |
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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 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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