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Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5

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, inflammatio...

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Autores principales: Cai, Zhengyao, Yuan, Suxin, Zhong, Yi, Deng, Li, Li, Jiafu, Tan, Xiaoqiu, Feng, Jian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8113688/
https://www.ncbi.nlm.nih.gov/pubmed/33995040
http://dx.doi.org/10.3389/fphar.2021.637051
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author Cai, Zhengyao
Yuan, Suxin
Zhong, Yi
Deng, Li
Li, Jiafu
Tan, Xiaoqiu
Feng, Jian
author_facet Cai, Zhengyao
Yuan, Suxin
Zhong, Yi
Deng, Li
Li, Jiafu
Tan, Xiaoqiu
Feng, Jian
author_sort Cai, Zhengyao
collection PubMed
description 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.
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spelling pubmed-81136882021-05-13 Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5 Cai, Zhengyao Yuan, Suxin Zhong, Yi Deng, Li Li, Jiafu Tan, Xiaoqiu Feng, Jian Front Pharmacol Pharmacology 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. Frontiers Media S.A. 2021-04-28 /pmc/articles/PMC8113688/ /pubmed/33995040 http://dx.doi.org/10.3389/fphar.2021.637051 Text en Copyright © 2021 Cai, Yuan, Zhong, Deng, Li, Tan and Feng. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Cai, Zhengyao
Yuan, Suxin
Zhong, Yi
Deng, Li
Li, Jiafu
Tan, Xiaoqiu
Feng, Jian
Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5
title Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5
title_full Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5
title_fullStr Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5
title_full_unstemmed Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5
title_short Amelioration of Endothelial Dysfunction in Diabetes: Role of Takeda G Protein–Coupled Receptor 5
title_sort amelioration of endothelial dysfunction in diabetes: role of takeda g protein–coupled receptor 5
topic Pharmacology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8113688/
https://www.ncbi.nlm.nih.gov/pubmed/33995040
http://dx.doi.org/10.3389/fphar.2021.637051
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