Abstract
Diabetes mellitus (DM) eventually leads to chronic vascular complications, resulting in cardiovascular diseases. DM-associated endothelial dysfunction (ED) plays an important role in the development of chronic vascular complications. Low endothelial nitric oxide synthase (eNOS) activity, inflammation, and oxidative stress all contribute to ED. The G protein–coupled receptor Takeda G protein–coupled receptor 5 (TGR5) is a membrane receptor for bile acids that plays an important role in the regulation of glucose metabolism. Recent studies have shown that TGR5 is involved in the regulation of various mediators of ED, which suggests that TGR5 may represent a target for the treatment of DM-associated ED. In this review, we summarize the principal mechanisms of DM-associated ED, then propose TGR5 as a novel therapeutic target on the basis of its mechanistic involvement, and suggest potential directions for future research.
Highlights
Diabetes mellitus (DM) is a global public health problem that is associated with a high financial burden for healthcare systems
We focus on the Endothelial dysfunction (ED) that develops in diabetes, because impairment in endothelial function usually develops before related complications manifest clinically; by reducing ED, we can minimize target organ damage, and by identifying ED, we may diagnose DM in asymptomatic individuals
Endothelial function is impaired in many tissues in diabetes and contributes to the impaired metabolic effects of insulin, as well as diabetic complications, and indicates that the endothelium is a potential target for the therapy of DM
Summary
Diabetes mellitus (DM) is a global public health problem that is associated with a high financial burden for healthcare systems. We focus on the ED that develops in diabetes, because impairment in endothelial function usually develops before related complications manifest clinically; by reducing ED, we can minimize target organ damage, and by identifying ED, we may diagnose DM in asymptomatic individuals. In most patients with DM, the goal of controlling cardiovascular disease (CVD) risk factors is not achieved, because hypoglycemic therapy alone does not seem to reduce the incidence of large vessel-related outcomes (Gerstein et al, 2008), and many of the drugs have side effects. In this review, we focus on ED and the role of TGR5 in DM, with the aim of collating evidence for this type of potential targeted therapy for DM
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