Recent advances in glucokinase activators for the treatment of type 2 diabetes

Recent advances in glucokinase activators for the treatment of type 2 diabetes Glucokinase is a member of the hexokinase family of enzymes that are responsible for the phosphorylation of glucose to glucose-6-phosphate for further utilization in cells. The enzyme plays a key role in glucose homeostasis. Phosphorylation of glucose by glucokinase in the liver promotes glycogen synthesis, while in the β-cell it results in insulin release. Activators of glucokinase increase the sensitivity of the enzyme to glucose, leading to increased insulin secretion and liver glycogen synthesis and a decrease in liver glucose output. Thus, small molecule glucokinase activators have been demonstrated to be effective glucose-lowering agents in animal models of type 2 diabetes and have advanced into clinical studies. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Drug Discovery Today Elsevier

Recent advances in glucokinase activators for the treatment of type 2 diabetes

Drug Discovery Today, Volume 14 (15) – Aug 1, 2009

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Publisher
Elsevier
Copyright
Copyright © 2009 Elsevier Ltd
ISSN
1359-6446
D.O.I.
10.1016/j.drudis.2009.05.013
Publisher site
See Article on Publisher Site

Abstract

Glucokinase is a member of the hexokinase family of enzymes that are responsible for the phosphorylation of glucose to glucose-6-phosphate for further utilization in cells. The enzyme plays a key role in glucose homeostasis. Phosphorylation of glucose by glucokinase in the liver promotes glycogen synthesis, while in the β-cell it results in insulin release. Activators of glucokinase increase the sensitivity of the enzyme to glucose, leading to increased insulin secretion and liver glycogen synthesis and a decrease in liver glucose output. Thus, small molecule glucokinase activators have been demonstrated to be effective glucose-lowering agents in animal models of type 2 diabetes and have advanced into clinical studies.

Journal

Drug Discovery TodayElsevier

Published: Aug 1, 2009

References

  • New perspectives on pancreatic islet glucokinase
    Meglasson, M.D.
  • Mammalian glucokinase
    Printz, R.G.
  • Predictive blood glucose lowering efficacy by glucokinase activators in high fat fed female Zucker rats
    Coope, G.J.
  • Discovery, synthesis and biological evaluation of novel glucokinase activators
    McKerrecher, D.
  • Glucokinase-activating ureas
    Castelhano, A.L.
  • Insulinotropic agent ID-1101 (4-hydroxyisoleucine) activates insulin signaling in rat
    Broca, C.

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