Glucokinase activators — a promising class of antidiabetic drugs
https://doi.org/10.14341/probl8747
Abstract
Type 2 diabetes mellitus is an urgent problem of the modern healthcare. Despite a wide choice of oral hypoglycemic drugs, today there is a great need to create and introduce into clinical practice new, effective, and safe drugs for the treatment of diabetes. One of the promising targets for the creation of new antidiabetics is a glucokinase. It has an exceptionally high influence on glucose homeostasis, serving as a glucose “sensor” in pancreatic β-cells and controlling the rate of glycogen synthesis in the liver. In the present work, the molecular-genetic structure of the enzyme, as well as its interrelation with the organs and tissues of the organism, is presented. The modern ideas about activators of glucokinase as a promising class of antidiabetic drugs are outlined, their hypoglycemic and general antidiabetic effects proved in preclinical and clinical studies are considered. The most advanced activators of glucokinase, undergoing clinical trials, are indicated.
About the Authors
Alexander A. SpasovVolgograd State Medical University
Russian Federation
MD, PhD, Professor
Vadim A. Kosolapov
Volgograd State Medical University
Russian Federation
MD, PhD, Professor
Denis A. Babkov
Volgograd State Medical University
Russian Federation
PhD
Olga Yu. Mayka
Volgograd State Medical University
Russian Federation
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Supplementary files
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1. Fig. 1. Organs and tissues expressing HA, and their relationship to each other. | |
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2. Fig. 2. Conformational cycles of glucokinase. | |
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3. Fig. 3. Participation of glucokinase in the regulation of β-cell mass. | |
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4. Fig. 4. Structural model of glucokinase. The centers of binding of activators of glucokinase and glucose are noted. | |
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5. Fig. 5. Mechanism of action of activators of glucokinase on the liver and pancreas. | |
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Review
For citations:
Spasov A.A., Kosolapov V.A., Babkov D.A., Mayka O.Yu. Glucokinase activators — a promising class of antidiabetic drugs. Problems of Endocrinology. 2018;64(3):180-187. https://doi.org/10.14341/probl8747
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