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Design, synthesis and SAR of novel glucokinase activators.

Cheruvallath ZS, Gwaltney SL, Sabat M, Tang M, Feng J, Wang H, Miura J, Guntupalli P, Jennings A, Hosfield D, Lee B, Wu Y
Bioorg Med Chem Lett 23 2166-71 (2013)
Related entries: 4ise, 4isf

Cited: 9 times
EuropePMC logo PMID: 23434031

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.

Articles - 4isg mentioned but not cited (1)

  1. Strain analysis of protein structures and low dimensionality of mechanical allosteric couplings. Mitchell MR, Tlusty T, Leibler S. Proc Natl Acad Sci U S A 113 E5847-E5855 (2016)


Reviews citing this publication (1)

  1. A report of 2 new cases of MODY2 and review of the literature: implications in the search for type 2 diabetes drugs. Shammas C, Neocleous V, Phelan MM, Lian LY, Skordis N, Phylactou LA. Metabolism 62 1535-1542 (2013)

Articles citing this publication (7)

  1. Structural insight into the glucokinase-ligands interactions. Molecular docking study. Ermakova E. Comput Biol Chem 64 281-296 (2016)
  2. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Cheruvallath ZS, Gwaltney SL, Sabat M, Tang M, Wang H, Jennings A, Hosfield D, Lee B, Wu Y, Halkowycz P, Grimshaw CE. Bioorg Med Chem Lett 27 2678-2682 (2017)
  3. Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose. Bowler JM, Hervert KL, Kearley ML, Miller BG. ACS Med Chem Lett 4 (2013)
  4. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Grewal AS, Kharb R, Prasad DN, Dua JS, Lather V. Chem Biol Drug Des 93 364-372 (2019)
  5. Comparative Efficacy of Adding Sitagliptin to Metformin, Sulfonylurea or Dual Therapy: A Propensity Score-Weighted Cohort Study. Mamza J, Mehta R, Donnelly R, Idris I. Diabetes Ther 6 213-226 (2015)
  6. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. Grewal AS, Kharb R, Prasad DN, Dua JS, Lather V. BMC Chem 13 2 (2019)
  7. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Dzyurkevich MS, Babkov DA, Shtyrlin NV, Mayka OY, Iksanova AG, Vassiliev PM, Balakin KV, Spasov AA, Tarasov VV, Barreto G, Shtyrlin YG, Aliev G. Sci Rep 7 16072 (2017)


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