Assessing the potential of glucokinase activators in diabetes therapy

Glucokinase, a unique isoform of the hexokinase enzymes, which are known to phosphorylate D-glucose and other hexoses, was identified during the past three to four decades as a new, promising drug target for type 2 diabetes. Glucokinase serves as a glucose sensor of the insulin-producing pancreatic...

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Bibliographic Details
Published inNature reviews. Drug discovery Vol. 8; no. 5; pp. 399 - 416
Main Author Matschinsky, Franz M
Format Journal Article
LanguageEnglish
Published England Nature Publishing Group 01.05.2009
Subjects
Animals
Blood Glucose - drug effects
Blood Glucose - metabolism
Carbohydrate metabolism
Care and treatment
Diabetes Mellitus, Type 2 - drug therapy
Diabetes Mellitus, Type 2 - enzymology
Enzyme Activation - drug effects
Enzyme Activation - physiology
Genetic aspects
Glucokinase
Glucokinase - metabolism
Humans
Hypoglycemic Agents - pharmacology
Hypoglycemic Agents - therapeutic use
Physiological aspects
Type 2 diabetes
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Summary:Glucokinase, a unique isoform of the hexokinase enzymes, which are known to phosphorylate D-glucose and other hexoses, was identified during the past three to four decades as a new, promising drug target for type 2 diabetes. Glucokinase serves as a glucose sensor of the insulin-producing pancreatic islet beta-cells, controls the conversion of glucose to glycogen in the liver and regulates hepatic glucose production. Guided by this fundamental knowledge, several glucokinase activators are now being developed, and have so far been shown to lower blood glucose in several animal models of type 2 diabetes and in initial trials in humans with the disease. Here, the scientific basis and current status of this new approach to diabetes therapy are discussed.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ObjectType-Review-1
ISSN:1474-1776
1474-1784
DOI:10.1038/nrd2850