Research Laboratory of Translational Medicine, Hengyang Medical School, University of South China, Hengyang, Hunan 421001, People's Republic of China.
Departments of Clinical Medicine, Hengyang Medical School, University of South China, Hengyang, Hunan 421001, People's Republic of China.
Biochem Cell Biol. 2024 Dec 1;102(6):418-429. doi: 10.1139/bcb-2024-0053. Epub 2024 Jul 16.
Atherosclerosis (AS) is an inflammatory arterial disorder that occurs due to the deposition of the excessive lipoprotein under the artery intima, mainly including low-density lipoprotein and other apolipoprotein B-containing lipoproteins. G protein-coupled receptors (GPCRs) play a crucial role in transmitting signals in physiological and pathophysiological conditions. GPCRs recognize inflammatory mediators, thereby serving as important players during chronic inflammatory processes. It has been demonstrated that free fatty acids can function as ligands for various GPCRs, such as free fatty acid receptor (FFAR)1/GPR40, FFAR2/GPR43, FFAR3/GPR41, FFAR4/GPR120, and the lipid metabolite binding glucose-dependent insulinotropic receptor (GPR119). This review discusses GPR43 and its ligands in the pathogenesis of AS, especially focusing on its distinct role in regulating chronic vascular inflammation, inhibiting oxidative stress, ameliorating endothelial dysfunction and improving dyslipidemia. It is hoped that this review may provide guidance for further studies aimed at GPR43 as a promising target for drug development in the prevention and therapy of AS.
动脉粥样硬化（AS）是一种炎症性动脉疾病，由于过量的脂蛋白在动脉内膜下沉积而发生，主要包括低密度脂蛋白和其他载脂蛋白 B 含脂蛋白。G 蛋白偶联受体（GPCRs）在生理和病理生理条件下传递信号中起着至关重要的作用。GPCRs 识别炎症介质，因此在慢性炎症过程中是重要的参与者。已经证明，游离脂肪酸可以作为各种 GPCR 的配体，例如游离脂肪酸受体（FFAR）1/GPR40、FFAR2/GPR43、FFAR3/GPR41、FFAR4/GPR120 和脂质代谢产物结合葡萄糖依赖性胰岛素释放受体（GPR119）。本综述讨论了 GPR43 及其在 AS 发病机制中的配体，特别是其在调节慢性血管炎症、抑制氧化应激、改善内皮功能障碍和改善血脂异常方面的独特作用。希望本综述可为进一步研究 GPR43 作为预防和治疗 AS 的有前途的药物靶点提供指导。
