Literature DB >> 21484569

SGLT inhibitors as new therapeutic tools in the treatment of diabetes.

Rolf K H Kinne1, Francisco Castaneda.   

Abstract

Recently, the idea has been developed to lower blood glucose blood glucose levels in diabetes by inhibiting sugar reabsorption sugar reabsorption in the kidney kidney . The main target is thereby the early proximal tubule proximal tubule where secondary active transport secondary active transport of the sugar is mediated by the sodium-D: -glucose D-glucose cotransporter SGLT2 SGLT2 . A model substance for the inhibitors inhibitors is the O-glucoside O-glucoside phlorizin phlorizin which inhibits transport transport competitively. Its binding to the transporter involves at least two different domains: an aglucone binding aglucone binding site at the transporter surface, involving extramembranous loops extramembraneous loops , and the sugar binding sugar binding /translocation site buried in a hydrophilic pocket of the transporter. The properties of these binding sites differ between SGLT2 and SGLT1 SGLT1 , which mediates sugar absorption sugar absorption in the intestine intestine . Various O-, C-, N- and S-glucosides have been synthesized with high affinity affinity and high specificity specificity for SGLT2 SGLT2 . Some of these glucosides are in clinical trials clinical trials and have been proven to successfully increase urinary glucose excretion urinary glucose excretion and to decrease blood sugar blood sugar levels without the danger of hypoglycaemia hypoglycaemia during fasting fasting in type 2 diabetes type 2 diabetes .

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Year:  2011        PMID: 21484569     DOI: 10.1007/978-3-642-17214-4_5

Source DB:  PubMed          Journal:  Handb Exp Pharmacol        ISSN: 0171-2004


  8 in total

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Journal:  Proc Natl Acad Sci U S A       Date:  2012-06-25       Impact factor: 11.205

2.  The Concise Guide to PHARMACOLOGY 2013/14: transporters.

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3.  Forces and dynamics of glucose and inhibitor binding to sodium glucose co-transporter SGLT1 studied by single molecule force spectroscopy.

Authors:  Isabel Neundlinger; Theeraporn Puntheeranurak; Linda Wildling; Christian Rankl; Lai-Xi Wang; Hermann J Gruber; Rolf K H Kinne; Peter Hinterdorfer
Journal:  J Biol Chem       Date:  2014-06-24       Impact factor: 5.157

4.  Phlorizin pretreatment reduces acute renal toxicity in a mouse model for diabetic nephropathy.

Authors:  Bas Brouwers; Vincent P E G Pruniau; Elisa J G Cauwelier; Frans Schuit; Evelyne Lerut; Nadine Ectors; Jeroen Declercq; John W M Creemers
Journal:  J Biol Chem       Date:  2013-08-11       Impact factor: 5.157

5.  New insight in understanding the contribution of SGLT1 in cardiac glucose uptake: evidence for a truncated form in mice and humans.

Authors:  Laura Ferté; Alice Marino; Sylvain Battault; Laurent Bultot; Anne Van Steenbergen; Anne Bol; Julien Cumps; Audrey Ginion; Hermann Koepsell; Laure Dumoutier; Louis Hue; Sandrine Horman; Luc Bertrand; Christophe Beauloye
Journal:  Am J Physiol Heart Circ Physiol       Date:  2021-01-08       Impact factor: 4.733

6.  Novel Strategies for the Treatment of COVID-19.

Authors:  Matthew W McCarthy
Journal:  Drugs R D       Date:  2022-08-24

7.  Role of macrophages in the altered epithelial function during a type 2 immune response induced by enteric nematode infection.

Authors:  Luigi Notari; Diana C Riera; Rex Sun; Jennifer A Bohl; Leon P McLean; Kathleen B Madden; Nico van Rooijen; Tim Vanuytsel; Joseph F Urban; Aiping Zhao; Terez Shea-Donohue
Journal:  PLoS One       Date:  2014-01-23       Impact factor: 3.240

Review 8.  A Beneficial Role of Rooibos in Diabetes Mellitus: A Systematic Review and Meta-Analysis.

Authors:  Moe Sasaki; Nami Nishida; Masako Shimada
Journal:  Molecules       Date:  2018-04-06       Impact factor: 4.411

  8 in total

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