| Target
Information |
| Name | mRNA of sodium-glucose transporter-2 |
| Type of target | Clinical trial target |
| Synonyms | mRNA of Low affinity sodium-glucose cotransporter |
| mRNA of Na(+)/glucose cotransporter 2 |
| mRNA of SGLT2 |
| mRNA of SLC5A2 |
| mRNA of Sodium/glucose cotransporter 2 |
| mRNA of Solute carrier family 5 member 2 |
| Disease | Type 2 Diabetes
[ICD9: 250.00, 250.02 ICD10: E11] | [1] |
| Drug(s) | ISIS-SGLT2 |  | Phase I | Type 2 Diabetes | [1] |
| UniProt ID | P31639 |
| Function | Sodium-dependent glucose transporter. Has a Na(+) to glucose coupling ratio of 1:1.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. |
| Sequence | MEEHTEAGSAPEMGAQKALIDNPADILVIAAYFLLVIGVGLWSMCRTNRGTVGGYFLAGR
SMVWWPVGASLFASNIGSGHFVGLAGTGAASGLAVAGFEWNALFVVLLLGWLFAPVYLTA
GVITMPQYLRKRFGGRRIRLYLSVLSLFLYIFTKISVDMFSGAVFIQQALGWNIYASVIA
LLGITMIYTVTGGLAALMYTDTVQTFVILGGACILMGYAFHEVGGYSGLFDKYLGAATSL
TVSEDPAVGNISSFCYRPRPDSYHLLRHPVTGDLPWPALLLGLTIVSGWYWCSDQVIVQR
CLAGKSLTHIKAGCILCGYLKLTPMFLMVMPGMISRILYPDEVACVVPEVCRRVCGTEVG
CSNIAYPRLVVKLMPNGLRGLMLAVMLAALMSSLASIFNSSSTLFTMDIYTRLRPRAGDR
ELLLVGRLWVVFIVVVSVAWLPVVQAAQGGQLFDYIQAVSSYLAPPVSAVFVLALFVPRV
NEQGAFWGLIGGLLMGLARLIPEFSFGSGSCVQPSACPAFLCGVHYLYFAIVLFFCSGLL
TLTVSLCTAPIPRKHLHRLVFSLRHSKEEREDLDADEQQGSSLPVQNGCPESAMEMNEPQ
APAPSLFRQCLLWFCGMSRGGVGSPPPLTQEEAAAAARRLEDISEDPSWARVVNLNALLM
MAVAVFLWGFYA
|
| Target Validation | Click to Find Target Validation Information. |
| Inhibitor | 10-methoxy-N (1)-methylburnamine-17-O-veratrate | | [2] |
| ACEROGENIN B | | [3] |
| Alstiphyllanine D | | [2] |
| Alstiphyllanine E | | [2] |
| Alstiphyllanine F | | [2] |
| Burnamine-17-O-3',4',5'-trimethoxybenzoate | | [2] |
| FORMONONETIN | | [4] |
| KURAIDIN | | [4] |
| KURARINONE | | [4] |
| MAACKIAIN | | [4] |
| O-spiroketal glucoside | | [5] |
| PHLORIZIN | | [6] |
| SERGLIFLOZIN A | | [7] |
| acerogenin C | | [3] |
| kushenol N | | [4] |
| remogliflozin | | [8] |
| sophoraflavanone G | | [4] |
| Antisense | ISIS-SGLT2 | | [1] |
| Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
| Ref 1 | 2011 Pipeline of ISIS Pharm. To Reference |
| Ref 2 | Bioorg Med Chem. 2010 Mar 15;18(6):2152-8. Epub 2010 Feb 6.Alstiphyllanines E-H, picraline and ajmaline-type alkaloids from Alstonia macrophylla inhibiting sodium glucose cotransporter. To Reference |
| Ref 3 | Bioorg Med Chem Lett. 2010 Feb 1;20(3):1070-4. Epub 2009 Dec 11.Cyclic diarylheptanoids as Na+-glucose cotransporter (SGLT) inhibitors from Acer nikoense. To Reference |
| Ref 4 | Bioorg Med Chem. 2007 May 15;15(10):3445-9. Epub 2007 Mar 12.Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens. To Reference |
| Ref 5 | Bioorg Med Chem. 2010 Jun 15;18(12):4422-32. Epub 2010 Apr 29.ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors. To Reference |
| Ref 6 | J Med Chem. 2010 Apr 22;53(8):3247-61.(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment. To Reference |
| Ref 7 | Bioorg Med Chem. 2010 Mar 15;18(6):2178-94. Epub 2010 Feb 4.Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners. To Reference |
| Ref 8 | J Med Chem. 2009 Apr 9;52(7):1785-94.Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2. To Reference |
