Literature DB >> 28045524

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.

Nicole C Goodwin1, Zhi-Ming Ding, Bryce A Harrison1, Eric D Strobel1, Angela L Harris, Melinda Smith, Andrea Y Thompson, Wendy Xiong, Faika Mseeh, Debra J Bruce, Damaris Diaz, Suma Gopinathan, Ling Li, Emily O'Neill, Mary Thiel, Alan G E Wilson, Kenneth G Carson1, David R Powell, David B Rawlins1.   

Abstract

The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodium-dependent glucose cotransporters (SGLT) have appeared as viable therapeutics to control blood glucose levels in diabetic patents. Herein we report the discovery of LX2761, a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.

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Year:  2017        PMID: 28045524     DOI: 10.1021/acs.jmedchem.6b01541

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  11 in total

Review 1.  Development of SGLT1 and SGLT2 inhibitors.

Authors:  Timo Rieg; Volker Vallon
Journal:  Diabetologia       Date:  2018-08-22       Impact factor: 10.122

Review 2.  Glucose transporters in the small intestine in health and disease.

Authors:  Hermann Koepsell
Journal:  Pflugers Arch       Date:  2020-08-23       Impact factor: 3.657

3.  What does sodium-glucose co-transporter 1 inhibition add: Prospects for dual inhibition.

Authors:  Jessica A Dominguez Rieg; Timo Rieg
Journal:  Diabetes Obes Metab       Date:  2019-04       Impact factor: 6.577

Review 4.  Novel and Unexpected Functions of SGLTs.

Authors:  Ernest M Wright; Chiara Ghezzi; Donald D F Loo
Journal:  Physiology (Bethesda)       Date:  2017-11

5.  SGLT1 and SGLT1 Inhibitors: A Role to Be Assessed in the Current Clinical Practice.

Authors:  Leonardo Spatola; Silvia Finazzi; Claudio Angelini; Marco Dauriz; Salvatore Badalamenti
Journal:  Diabetes Ther       Date:  2017-11-24       Impact factor: 2.945

Review 6.  Predicting human disease mutations and identifying drug targets from mouse gene knockout phenotyping campaigns.

Authors:  Robert Brommage; David R Powell; Peter Vogel
Journal:  Dis Model Mech       Date:  2019-05-07       Impact factor: 5.758

7.  High-Throughput Screening of Mouse Gene Knockouts Identifies Established and Novel High Body Fat Phenotypes.

Authors:  David R Powell; Jean-Pierre Revelli; Deon D Doree; Christopher M DaCosta; Urvi Desai; Melanie K Shadoan; Lawrence Rodriguez; Michael Mullens; Qi M Yang; Zhi-Ming Ding; Laura L Kirkpatrick; Peter Vogel; Brian Zambrowicz; Arthur T Sands; Kenneth A Platt; Gwenn M Hansen; Robert Brommage
Journal:  Diabetes Metab Syndr Obes       Date:  2021-08-28       Impact factor: 3.168

Review 8.  Intestinal Saturated Long-Chain Fatty Acid, Glucose and Fructose Transporters and Their Inhibition by Natural Plant Extracts in Caco-2 Cells.

Authors:  Katharina Schreck; Matthias F Melzig
Journal:  Molecules       Date:  2018-10-06       Impact factor: 4.411

9.  Novel natural and synthetic inhibitors of solute carriers SGLT1 and SGLT2.

Authors:  Paul Oranje; Robin Gouka; Lindsey Burggraaff; Mario Vermeer; Clément Chalet; Guus Duchateau; Pieter van der Pijl; Marian Geldof; Niels de Roo; Fenja Clauwaert; Toon Vanpaeschen; Johan Nicolaï; Tom de Bruyn; Pieter Annaert; Adriaan P IJzerman; Gerard J P van Westen
Journal:  Pharmacol Res Perspect       Date:  2019-07-30

10.  Sotagliflozin Decreases Postprandial Glucose and Insulin Concentrations by Delaying Intestinal Glucose Absorption.

Authors:  David R Powell; Brian Zambrowicz; Linda Morrow; Carine Beysen; Marcus Hompesch; Scott Turner; Marc Hellerstein; Phillip Banks; Paul Strumph; Pablo Lapuerta
Journal:  J Clin Endocrinol Metab       Date:  2020-04-01       Impact factor: 5.958

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