Literature DB >> 23434031

Design, synthesis and SAR of novel glucokinase activators.

Zacharia S Cheruvallath1, Stephen L Gwaltney, Mark Sabat, Mingnam Tang, Jun Feng, Haixia Wang, Joanne Miura, Prasuna Guntupalli, Andy Jennings, David Hosfield, Bumsup Lee, Yiqin Wu.   

Abstract

Guided by co-crystal structures of compounds 15, 22 and 30, an SBDD approach led to the discovery of the 6-methyl pyridone series as a novel class of GKAs that potently activate GK in enzyme and cell assays. Anti-diabetic OGTT efficacy was demonstrated with 54 in a mouse model of type 2 diabetes.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23434031     DOI: 10.1016/j.bmcl.2013.01.093

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Strain analysis of protein structures and low dimensionality of mechanical allosteric couplings.

Authors:  Michael R Mitchell; Tsvi Tlusty; Stanislas Leibler
Journal:  Proc Natl Acad Sci U S A       Date:  2016-09-21       Impact factor: 11.205

2.  Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose.

Authors:  Joseph M Bowler; Katherine L Hervert; Mark L Kearley; Brian G Miller
Journal:  ACS Med Chem Lett       Date:  2013-09-05       Impact factor: 4.345

3.  Comparative Efficacy of Adding Sitagliptin to Metformin, Sulfonylurea or Dual Therapy: A Propensity Score-Weighted Cohort Study.

Authors:  Jil Mamza; Rajnikant Mehta; Richard Donnelly; Iskandar Idris
Journal:  Diabetes Ther       Date:  2015-05-27       Impact factor: 2.945

4.  Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus.

Authors:  Mikhail S Dzyurkevich; Denis A Babkov; Nikita V Shtyrlin; Olga Yu Mayka; Alfiya G Iksanova; Pavel M Vassiliev; Konstantin V Balakin; Alexander A Spasov; Vadim V Tarasov; George Barreto; Yurii G Shtyrlin; Gjumrakch Aliev
Journal:  Sci Rep       Date:  2017-11-22       Impact factor: 4.379

  4 in total

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