Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T30085
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| Former ID |
TTDNC00579
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| Target Name |
SLGT2
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| Gene Name |
SLC5A2
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| Synonyms |
Low affinity sodium-glucose cotransporter; Na(+)/glucose cotransporter 2; Sodium/glucose cotransporter 2; Solute carrier family 5 member 2; SLC5A2
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| Target Type |
Successful
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| Disease | Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | ||||
| Liver disease [ICD9: 570-574; ICD10: K70-K77] | |||||
| Type 2 diabetes [ICD9: 250; ICD10: E11] | |||||
| Type 1 diabetes [ICD9: 250; ICD10: E10] | |||||
| Function |
Efficient substrate transport in mammalian kidney is provided by the concerted action of a low affinity high capacity and a high affinity low capacity Na(+)/glucose cotransporter arranged in series along kidney proximal tubules.
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| BioChemical Class |
Solute:sodium symporter
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| UniProt ID | |||||
| Sequence |
MEEHTEAGSAPEMGAQKALIDNPADILVIAAYFLLVIGVGLWSMCRTNRGTVGGYFLAGR
SMVWWPVGASLFASNIGSGHFVGLAGTGAASGLAVAGFEWNALFVVLLLGWLFAPVYLTA GVITMPQYLRKRFGGRRIRLYLSVLSLFLYIFTKISVDMFSGAVFIQQALGWNIYASVIA LLGITMIYTVTGGLAALMYTDTVQTFVILGGACILMGYAFHEVGGYSGLFDKYLGAATSL TVSEDPAVGNISSFCYRPRPDSYHLLRHPVTGDLPWPALLLGLTIVSGWYWCSDQVIVQR CLAGKSLTHIKAGCILCGYLKLTPMFLMVMPGMISRILYPDEVACVVPEVCRRVCGTEVG CSNIAYPRLVVKLMPNGLRGLMLAVMLAALMSSLASIFNSSSTLFTMDIYTRLRPRAGDR ELLLVGRLWVVFIVVVSVAWLPVVQAAQGGQLFDYIQAVSSYLAPPVSAVFVLALFVPRV NEQGAFWGLIGGLLMGLARLIPEFSFGSGSCVQPSACPAFLCGVHYLYFAIVLFFCSGLL TLTVSLCTAPIPRKHLHRLVFSLRHSKEEREDLDADEQQGSSLPVQNGCPESAMEMNEPQ APAPSLFRQCLLWFCGMSRGGVGSPPPLTQEEAAAAARRLEDISEDPSWARVVNLNALLM MAVAVFLWGFYA |
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| Drugs and Mode of Action | |||||
| Drug(s) | Canagliflozin | Drug Info | Approved | Type 2 diabetes | [1], [2], [3] |
| Dapagliflozin | Drug Info | Approved | Type 2 diabetes | [4], [5] | |
| Dapagliflozin Propanediol; Saxagliptin Hydrochloride | Drug Info | Approved | Type 2 diabetes | [6] | |
| Empagliflozin | Drug Info | Approved | Type 1 diabetes | [7], [5] | |
| ASP1941 | Drug Info | Phase 3 | Liver disease | [8] | |
| PF-04971729 | Drug Info | Phase 3 | Type 2 diabetes | [9] | |
| AVE-2268 | Drug Info | Phase 2 | Diabetes | [10] | |
| Canagliflozin | Drug Info | Phase 2 | Type 2 diabetes | [1], [11] | |
| LX-4211 | Drug Info | Phase 2 | Type 2 diabetes | [12], [13] | |
| RO-4998452 | Drug Info | Phase 2 | Type 2 diabetes | [14] | |
| YM-543 | Drug Info | Phase 2 | Type 2 diabetes | [15] | |
| BI-44847 | Drug Info | Phase 1 | Type 2 diabetes | [16] | |
| EGT-0001474 | Drug Info | Phase 1 | Type 2 diabetes | [17] | |
| TS-033 | Drug Info | Discontinued in Phase 2 | Diabetes | [18] | |
| Modulator | ASP1941 | Drug Info | |||
| AVE-2268 | Drug Info | [19] | |||
| BI-44847 | Drug Info | ||||
| Canagliflozin | Drug Info | [2], [3] | |||
| Dapagliflozin | Drug Info | [5] | |||
| Dapagliflozin Propanediol; Saxagliptin Hydrochloride | Drug Info | [20] | |||
| EGT-0001474 | Drug Info | ||||
| Empagli ozin | Drug Info | [5] | |||
| Empagliflozin | Drug Info | [5] | |||
| LX-4211 | Drug Info | [21] | |||
| PF-04971729 | Drug Info | ||||
| RO-4998452 | Drug Info | ||||
| TS-033 | Drug Info | ||||
| YM-543 | Drug Info | ||||
| Inhibitor | sergliflozin | Drug Info | [22] | ||
| Pathways | |||||
| Reactome | Hexose transport | ||||
| Na+-dependent glucose transporters | |||||
| Inositol transporters | |||||
| WikiPathways | NRF2 pathway | ||||
| Nuclear Receptors Meta-Pathway | |||||
| Transport of glucose and other sugars, bile salts and organic acids, metal ions and amine compounds | |||||
| References | |||||
| REF 1 | (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: 4582). | ||||
| REF 2 | 2013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9. | ||||
| REF 3 | Canagliflozin, a sodium glucose co-transporter 2 inhibitor, reduces post-meal glucose excursion in patients with type 2 diabetes by a non-renal mechanism: results of a randomized trial. Metabolism. 2014 Oct;63(10):1296-303. | ||||
| REF 4 | (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: 4594). | ||||
| REF 5 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | ||||
| REF 6 | Drugs@FDA (Edaravone) | ||||
| REF 7 | (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: 4754). | ||||
| REF 8 | ClinicalTrials.gov (NCT01054092) A Study to Assess the Long-term Safety and Efficacy of ASP1941 in Japanese Diabetic Patients. U.S. National Institutes of Health. | ||||
| REF 9 | ClinicalTrials.gov (NCT02226003) Efficacy and Safety of Ertugliflozin (MK-8835/PF-04971729) With Sitagliptin in the Treatment of Participants With Type 2 Diabetes Mellitus (T2DM) With Inadequate Glycemic Control on Diet and Exercise (MK-8835-017). U.S. National Institutes of Health. | ||||
| REF 10 | ClinicalTrials.gov (NCT00361738) Dose-Ranging Study Evaluating AVE2268 in Patients With Type 2 Diabetes Not Adequately Controlled by a Metformin Treatment. U.S. National Institutes of Health. | ||||
| REF 11 | Clinical pipeline report, company report or official report of Johnson & Johnson (2011). | ||||
| REF 12 | ClinicalTrials.gov (NCT01742208) Safety and Efficacy of LX4211 in Patients With Inadequately Controlled Type 1 Diabetes Mellitus. U.S. National Institutes of Health. | ||||
| REF 13 | (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: 8312). | ||||
| REF 14 | ClinicalTrials.gov (NCT00800176) A Dose-Finding Study of RO4998452 in Patients With Diabetes Mellitus. U.S. National Institutes of Health. | ||||
| REF 15 | ClinicalTrials.gov (NCT00454233) A Safety and Efficacy Study With YM543 in Type 2 Diabetes Mellitus Subjects. U.S. National Institutes of Health. | ||||
| REF 16 | ClinicalTrials.gov (NCT02211937) Relative Oral Bioavailability of BI 44847 as Suspension Compared to Tablet and the Influence of Food Anf of BI 44847 as Solution Compared to Tablet in Healthy Male Volunteers. U.S. National Institutes of Health. | ||||
| REF 17 | ClinicalTrials.gov (NCT00854113) Study to Determine the Safety, Tolerability, and Pharmacokinetic (PK) Profile of EGT0001474 in Healthy Volunteers. U.S. National Institutes of Health. | ||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021799) | ||||
| REF 19 | Effects of AVE2268, a substituted glycopyranoside, on urinary glucose excretion and blood glucose in mice and rats. Arzneimittelforschung. 2008;58(11):574-80. | ||||
| REF 20 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
| REF 21 | LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin Pharmacol Ther. 2012 Aug;92(2):158-69. | ||||
| REF 22 | Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level. J Pharmacol Exp Ther. 2007 Jan;320(1):323-30. Epub 2006 Oct 18. | ||||
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