Metabolite G-Protein Coupled Receptors in Cardio-Metabolic Diseases.

Metabolite G-Protein Coupled Receptors in Cardio-Metabolic Diseases.
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DOI:
10.3390/cells10123347
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发表时间:
2021-11-29
期刊:
影响因子:
6
通讯作者:
Karoor V
Karoor V
中科院分区:
生物学2区
文献类型:
--
作者:
Strassheim D;Sullivan T;Irwin DC;Gerasimovskaya E;Lahm T;Klemm DJ;Dempsey EC;Stenmark KR;Karoor V

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G蛋白偶联受体(GPCR)最初被描述为由激素、神经递质和其他介质激活的受体家族。然而,近年来,GPCR已显示结合内源性代谢物,其除了作为信号传导介质之外还发挥功能。这些受体对脂肪酸、单糖和二糖、氨基酸或各种代谢中间体和产物(包括酮体、乳酸盐、琥珀酸盐或胆汁酸)作出反应。鉴于这些代谢过程中的许多在病理条件下失调,包括糖尿病、血脂异常和肥胖症,内源性代谢物的受体也被认为是预防和/或治疗代谢和心血管疾病的潜在药物靶标。本文综述了内源性代谢产物激活的G蛋白偶联受体及其生理、病理生理和潜在的药理作用。
G protein-coupled receptors (GPCRs) have originally been described as a family of receptors activated by hormones, neurotransmitters, and other mediators. However, in recent years GPCRs have shown to bind endogenous metabolites, which serve functions other than as signaling mediators. These receptors respond to fatty acids, mono- and disaccharides, amino acids, or various intermediates and products of metabolism, including ketone bodies, lactate, succinate, or bile acids. Given that many of these metabolic processes are dysregulated under pathological conditions, including diabetes, dyslipidemia, and obesity, receptors of endogenous metabolites have also been recognized as potential drug targets to prevent and/or treat metabolic and cardiovascular diseases. This review describes G protein-coupled receptors activated by endogenous metabolites and summarizes their physiological, pathophysiological, and potential pharmacological roles.
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