Glucokinase activators — a promising class of antidiabetic drugs

A. Spasov, Спасов Александр Алексеевич, V. Kosolapov, Косолапов Вадим Анатольевич, D. Babkov, Бабков Денис Александрович, O. Mayka, Майка Ольга Юрьевна
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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.
葡萄糖激酶激活剂——一类很有前途的抗糖尿病药物
2型糖尿病是现代医疗保健领域亟待解决的问题。尽管口服降糖药的选择范围很广,但今天仍然非常需要创造新的、有效的、安全的治疗糖尿病的药物并将其引入临床实践。创造新的抗糖尿病药物的一个有希望的目标是葡萄糖激酶。它对葡萄糖稳态有特别高的影响,在胰腺β细胞中作为葡萄糖“传感器”并控制肝脏中糖原合成的速率。在目前的工作中,介绍了酶的分子遗传结构,以及它与生物体器官和组织的相互关系。概述了葡萄糖激酶活化剂作为一类很有前途的降糖药物的现代观点,并对其在临床前和临床研究中证实的降糖和一般降糖作用进行了评述。最先进的葡萄糖激酶活化剂,正在进行临床试验,指出。
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