| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T54771 | ||||
| Target Name | Sodium/glucose cotransporter 1 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | QSPac | Drug Info | IC50 = 0.17 nM | [528982] | |
| Sophoraflavanone G | Drug Info | IC50 = 18700 nM | [528742] | ||
| O-spiroketal glucoside | Drug Info | IC50 = 1300 nM | [530988] | ||
| KURARINONE | Drug Info | IC50 = 10400 nM | [528742] | ||
| QCP | Drug Info | IC50 = 2.1 nM | [528982] | ||
| Action against Disease Model | Phlorizin | The phlorizin binding properties of l uMinal membrane vesicles isolated from the LLC-PK1 cells, a continuous epithelial cell line derived from pig kidney, are studied. Scatchardanalysis of this binding indicates the existence of a single high affinity sodi uM-dependent site with KD = 0.4 microM at 266 mM sodi uM. | [533444] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Here, we show that the sweet taste receptor subunit T1R3 and the taste G protein gustducin, expressed in enteroendocrine cells, underlie intestinal sugar sensing and regulation of SGLT1 mRNA and protein. Dietary sugar and artificial sweeteners increased SGLT1 mRNA and protein expression, and glucose absorptive capacity in wild-type mice, but not in knockout mice lacking T1R3or alpha-gustducin. Artificial sweeteners, acting on sweet taste receptors expressed on enteroendocrine GLUTag cells, stimulated secretion of gut hormones implicated in SGLT1 up-regulation. Gut-expressed taste signaling elements involved in regulating SGLT1 expression could provide novel therapeutic targets for modulating the gut's capacity to absorb sugars, with implications for the prevention and/or treatment of malabsorption syndromes and diet-related disorders including diabetes and obesity | [528982] | |||
| References | |||||
| Ref 528982 | J Biol Chem. 2007 Sep 28;282(39):28501-13. Epub 2007 Aug 8.Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity. | ||||
| Ref 528742 | 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. | ||||
| Ref 530988 | 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. | ||||
| Ref 528742 | 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. | ||||
| Ref 528982 | J Biol Chem. 2007 Sep 28;282(39):28501-13. Epub 2007 Aug 8.Tripeptides of RS1 (RSC1A1) inhibit a monosaccharide-dependent exocytotic pathway of Na+-D-glucose cotransporter SGLT1 with high affinity. | ||||
| Ref 533444 | J Biol Chem. 1988 Jan 5;263(1):187-92.High affinity phlorizin binding to the LLC-PK1 cells exhibits a sodium:phlorizin stoichiometry of 2:1. | ||||
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