Literature DB >> 18260618

Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

Wei Meng1, Bruce A Ellsworth, Alexandra A Nirschl, Peggy J McCann, Manorama Patel, Ravindar N Girotra, Gang Wu, Philip M Sher, Eamonn P Morrison, Scott A Biller, Robert Zahler, Prashant P Deshpande, Annie Pullockaran, Deborah L Hagan, Nathan Morgan, Joseph R Taylor, Mary T Obermeier, William G Humphreys, Ashish Khanna, Lorell Discenza, James G Robertson, Aiying Wang, Songping Han, John R Wetterau, Evan B Janovitz, Oliver P Flint, Jean M Whaley, William N Washburn.   

Abstract

The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2 diabetes.

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Year:  2008        PMID: 18260618     DOI: 10.1021/jm701272q

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


  106 in total

Review 1.  Sodium-glucose transport: role in diabetes mellitus and potential clinical implications.

Authors:  Volker Vallon; Kumar Sharma
Journal:  Curr Opin Nephrol Hypertens       Date:  2010-09       Impact factor: 2.894

2.  A fluorescence method for measurement of glucose transport in kidney cells.

Authors:  Amy B Blodgett; Rajendra K Kothinti; Ivan Kamyshko; David H Petering; Suresh Kumar; Niloofar M Tabatabai
Journal:  Diabetes Technol Ther       Date:  2011-04-21       Impact factor: 6.118

3.  A tool for multi-scale modelling of the renal nephron.

Authors:  David P Nickerson; Jonna R Terkildsen; Kirk L Hamilton; Peter J Hunter
Journal:  Interface Focus       Date:  2011-03-30       Impact factor: 3.906

Review 4.  SGLT2 inhibition--a novel strategy for diabetes treatment.

Authors:  Edward C Chao; Robert R Henry
Journal:  Nat Rev Drug Discov       Date:  2010-05-28       Impact factor: 84.694

5.  Total synthesis of (+)-scholarisine A.

Authors:  Gregory L Adams; Patrick J Carroll; Amos B Smith
Journal:  J Am Chem Soc       Date:  2012-01-25       Impact factor: 15.419

Review 6.  SGLT2 inhibition in diabetes mellitus: rationale and clinical prospects.

Authors:  Ele Ferrannini; Anna Solini
Journal:  Nat Rev Endocrinol       Date:  2012-02-07       Impact factor: 43.330

7.  Present and Prospective Pharmacotherapy for the Management of Patients with Type 2 Diabetes.

Authors:  Leonor Corsino; Mary Elizabeth Cox; Jennifer Rowel; Jennifer B Green
Journal:  Clin Med Ther       Date:  2009-08-27

Review 8.  Renal glucose transporters: novel targets for hyperglycemia management.

Authors:  Amanda Mather; Carol Pollock
Journal:  Nat Rev Nephrol       Date:  2010-03-30       Impact factor: 28.314

Review 9.  Incretins and selective renal sodium-glucose co-transporter 2 inhibitors in hypertension and coronary heart disease.

Authors:  Ramiro A Sanchez; Hugo Sanabria; Cecilia de Los Santos; Agustin J Ramirez
Journal:  World J Diabetes       Date:  2015-09-10

10.  Dapagliflozin Binds Specifically to Sodium-Glucose Cotransporter 2 in the Proximal Renal Tubule.

Authors:  Chiara Ghezzi; Amy S Yu; Bruce A Hirayama; Vladimir Kepe; Jie Liu; Claudio Scafoglio; David R Powell; Sung-Cheng Huang; Nagichettiar Satyamurthy; Jorge R Barrio; Ernest M Wright
Journal:  J Am Soc Nephrol       Date:  2016-09-12       Impact factor: 10.121

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