Target Information

Target General Infomation
Target ID
T30085
Former ID
TTDNC00579
Target Name
SLGT2
Gene Name
SLC5A2
Synonyms
Low affinity sodium-glucose cotransporter; Na(+)/glucose cotransporter 2; Sodium/glucose cotransporter 2; Solute carrier family 5 member 2; SLC5A2
Target Type
Successful
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.
BioChemical Class
Solute:sodium symporter
UniProt ID
P31639
Sequence
MEEHTEAGSAPEMGAQKALIDNPADILVIAAYFLLVIGVGLWSMCRTNRGTVGGYFLAGR
SMVWWPVGASLFASNIGSGHFVGLAGTGAASGLAVAGFEWNALFVVLLLGWLFAPVYLTA
GVITMPQYLRKRFGGRRIRLYLSVLSLFLYIFTKISVDMFSGAVFIQQALGWNIYASVIA
LLGITMIYTVTGGLAALMYTDTVQTFVILGGACILMGYAFHEVGGYSGLFDKYLGAATSL
TVSEDPAVGNISSFCYRPRPDSYHLLRHPVTGDLPWPALLLGLTIVSGWYWCSDQVIVQR
CLAGKSLTHIKAGCILCGYLKLTPMFLMVMPGMISRILYPDEVACVVPEVCRRVCGTEVG
CSNIAYPRLVVKLMPNGLRGLMLAVMLAALMSSLASIFNSSSTLFTMDIYTRLRPRAGDR
ELLLVGRLWVVFIVVVSVAWLPVVQAAQGGQLFDYIQAVSSYLAPPVSAVFVLALFVPRV
NEQGAFWGLIGGLLMGLARLIPEFSFGSGSCVQPSACPAFLCGVHYLYFAIVLFFCSGLL
TLTVSLCTAPIPRKHLHRLVFSLRHSKEEREDLDADEQQGSSLPVQNGCPESAMEMNEPQ
APAPSLFRQCLLWFCGMSRGGVGSPPPLTQEEAAAAARRLEDISEDPSWARVVNLNALLM
MAVAVFLWGFYA
Drugs and Mode of Action
Drug(s) Canagliflozin Drug Info Approved Type 2 diabetes [467821], [532651], [532916]
Dapagliflozin Drug Info Approved Type 2 diabetes [467834], [533123]
Dapagliflozin Propanediol; Saxagliptin Hydrochloride Drug Info Approved Type 2 diabetes [889446]
Empagliflozin Drug Info Approved Type 1 diabetes [467995], [533123]
ASP1941 Drug Info Phase 3 Liver disease [522923]
PF-04971729 Drug Info Phase 3 Type 2 diabetes [524892]
AVE-2268 Drug Info Phase 2 Diabetes [521866]
Canagliflozin Drug Info Phase 2 Type 2 diabetes [467821], [551060]
LX-4211 Drug Info Phase 2 Type 2 diabetes [524151], [543064]
RO-4998452 Drug Info Phase 2 Type 2 diabetes [522503]
YM-543 Drug Info Phase 2 Type 2 diabetes [521996]
BI-44847 Drug Info Phase 1 Type 2 diabetes [524868]
EGT-0001474 Drug Info Phase 1 Type 2 diabetes [522600]
TS-033 Drug Info Discontinued in Phase 2 Diabetes [548084]
Modulator ASP1941 Drug Info
AVE-2268 Drug Info [529915]
BI-44847 Drug Info
Canagliflozin Drug Info [532651], [532916]
Dapagliflozin Drug Info [533123]
Dapagliflozin Propanediol; Saxagliptin Hydrochloride Drug Info [556264]
EGT-0001474 Drug Info
Empagli ozin Drug Info [533123]
Empagliflozin Drug Info [533123]
LX-4211 Drug Info [531953]
PF-04971729 Drug Info
RO-4998452 Drug Info
TS-033 Drug Info
YM-543 Drug Info
Inhibitor sergliflozin Drug Info [528482]
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 467821(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 467834(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 467995(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 521866ClinicalTrials.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 521996ClinicalTrials.gov (NCT00454233) A Safety and Efficacy Study With YM543 in Type 2 Diabetes Mellitus Subjects. U.S. National Institutes of Health.
Ref 522503ClinicalTrials.gov (NCT00800176) A Dose-Finding Study of RO4998452 in Patients With Diabetes Mellitus. U.S. National Institutes of Health.
Ref 522600ClinicalTrials.gov (NCT00854113) Study to Determine the Safety, Tolerability, and Pharmacokinetic (PK) Profile of EGT0001474 in Healthy Volunteers. U.S. National Institutes of Health.
Ref 522923ClinicalTrials.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 524151ClinicalTrials.gov (NCT01742208) Safety and Efficacy of LX4211 in Patients With Inadequately Controlled Type 1 Diabetes Mellitus. U.S. National Institutes of Health.
Ref 524868ClinicalTrials.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 524892ClinicalTrials.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 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 532916Canagliflozin, 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 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 543064(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 548084Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021799)
Ref 551060Clinical pipeline report, company report or official report of Johnson & Johnson (2011).
Ref 889446Drugs@FDA (Edaravone)
Ref 528482Sergliflozin, 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.
Ref 529915Effects of AVE2268, a substituted glycopyranoside, on urinary glucose excretion and blood glucose in mice and rats. Arzneimittelforschung. 2008;58(11):574-80.
Ref 531953LX4211, 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 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 532916Canagliflozin, 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 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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