期刊
EXPERT OPINION ON INVESTIGATIONAL DRUGS
卷 10, 期 3, 页码 439-454出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543784.10.3.439
关键词
antihyperglycaemic; blood glucose; diabetic animal models; diabetic complications; drug discovery; enzyme; gluconeogenesis; glycogen phosphorylase inhibitor; glycogenolysis; hepatic glucose production; indole inhibitor site; myocardial infarction; obesity; oral hypoglycaemic agents; stroke; type 2 diabetes mellitus therapy
Type 2 diabetes mellitus is a severe disease with large economic consequences. which is significantly under-diagnosed and incompletely treated in the general population. Control of blood glucose levels: is 3 key objective in treating diabetic patients, who are most often prescribed one or more oral hypoglycaemic agents in addition to diet and exercise modification as well as insulin. In spite of the availability of different classes of hypoglycaemic drugs, treatment regimens are often unable to achieve an intensive degree of glucose control known to must effectively reduce the incidence and severity of diabetic complications. Hepatic glucose output is elevated in type 2 diabetic patients and current evidence indicates that glycogenolysis (release of monomeric glucose front the glycogen polymer storage form) is an important contributor to the;abnormally high production of glucose by the liver. Glycogen phosphorylase is the enzyme that catalyses this release and recent advances in new. inhibitors of this structurally and kinetically well studied enzyme have enabled work which further delineate the pharmacological and physiological consequences of inhihiting glucose production by this pathway, Most notably, these agents lower glucose in diabetic animal models, both acutely and chronically, appear to affect both gluconeogenic and glycogenolytic pathways and demonstrate potential for a beneficial effect on cardiovascular risk factors. Cumulatively. this information has bolstered interest and promise in glycogen phosphorylase inhibitors (GPIs) as potential new hypoglycaemic agents fur treatment of type 2 diabetes mellitus.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据