Abstract
Glucokinase (GK) is a molecular sensor that regulates glucose induced insulin secretion in pancreatic β-cells and glucose homeostasis in the liver via catalysis of glucose to glucose-6-phosphate. The recent discovery and development of small molecule glucokinase activators represents a potentially important development for the management of type 2 diabetes. Since the discovery of the first orally active small molecule GK activator RO0281675, a number of research groups have reported the identification of potent activators. In this review, the biological significance of GK in whole body glucose homeostasis is briefly described coupled with the recent progress regarding the identification of novel small molecule GK activators.
Keywords: Glucokinase activator, permanent neonatal diabetes mellitus (PNDM), RO0281675, spirocyclopropane, nicotinamide
Current Medicinal Chemistry
Title: Small Molecule Glucokinase Activators as Glucose Lowering Agents: A New Paradigm for Diabetes Therapy
Volume: 13 Issue: 15
Author(s): Kevin R. Guertin and Joseph Grimsby
Affiliation:
Keywords: Glucokinase activator, permanent neonatal diabetes mellitus (PNDM), RO0281675, spirocyclopropane, nicotinamide
Abstract: Glucokinase (GK) is a molecular sensor that regulates glucose induced insulin secretion in pancreatic β-cells and glucose homeostasis in the liver via catalysis of glucose to glucose-6-phosphate. The recent discovery and development of small molecule glucokinase activators represents a potentially important development for the management of type 2 diabetes. Since the discovery of the first orally active small molecule GK activator RO0281675, a number of research groups have reported the identification of potent activators. In this review, the biological significance of GK in whole body glucose homeostasis is briefly described coupled with the recent progress regarding the identification of novel small molecule GK activators.
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Cite this article as:
Guertin R. Kevin and Grimsby Joseph, Small Molecule Glucokinase Activators as Glucose Lowering Agents: A New Paradigm for Diabetes Therapy, Current Medicinal Chemistry 2006; 13 (15) . https://dx.doi.org/10.2174/092986706777452551
DOI https://dx.doi.org/10.2174/092986706777452551 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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