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一种烟酸受体的鉴定:这是最古老的降脂药物的分子靶点吗?

Identification of a nicotinic acid receptor: is this the molecular target for the oldest lipid-lowering drug?

作者信息

Pike Nicholas B, Wise Alan

机构信息

Cardiovascular and Urogenital Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK.

出版信息

Curr Opin Investig Drugs. 2004 Mar;5(3):271-5.

PMID:15083592
Abstract

Nicotinic acid has been used clinically for over 40 years in the treatment of dyslipidemia, producing a desirable normalization of a range of cardiovascular risk factors. The precise mechanism of action of nicotinic acid is unknown, although it is believed that activation of a Gi-type G protein-coupled receptor, resulting in the inhibition of adipocyte lipolysis, may contribute. This review describes the identification of this elusive receptor, and outlines the evidence suggesting that this may be the molecular target for the clinical effects of nicotinic acid.

摘要

烟酸已在临床上用于治疗血脂异常40多年,可使一系列心血管危险因素实现理想的正常化。尽管人们认为激活一种Gi型G蛋白偶联受体,从而抑制脂肪细胞脂解可能起了作用,但烟酸的确切作用机制尚不清楚。这篇综述描述了这种难以捉摸的受体的鉴定过程,并概述了表明其可能是烟酸临床效应分子靶点的证据。

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1
Identification of a nicotinic acid receptor: is this the molecular target for the oldest lipid-lowering drug?一种烟酸受体的鉴定:这是最古老的降脂药物的分子靶点吗?
Curr Opin Investig Drugs. 2004 Mar;5(3):271-5.
2
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引用本文的文献

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Deficiency of metabolite sensing receptor HCA2 impairs the salutary effect of niacin in hemorrhagic shock.代谢物感应受体 HCA2 的缺乏会损害烟酸在失血性休克中的有益作用。
Biochim Biophys Acta Mol Basis Dis. 2019 Mar 1;1865(3):688-695. doi: 10.1016/j.bbadis.2019.01.009. Epub 2019 Jan 6.
2
Lipolytic actions of secretin in mouse adipocytes.促胰液素对小鼠脂肪细胞的脂解作用。
J Lipid Res. 2014 Feb;55(2):190-200. doi: 10.1194/jlr.M038042. Epub 2013 Nov 22.
3
Extended release niacin-laropiprant in patients with hypercholesterolemia or mixed dyslipidemias improves clinical parameters.
对于高胆固醇血症或混合型血脂异常患者,缓释烟酸-拉罗匹仑可改善临床指标。
Clin Med Insights Cardiol. 2011;5:85-101. doi: 10.4137/CMC.S7601. Epub 2011 Sep 19.
4
Mechanisms of flushing due to niacin and abolition of these effects.烟酸引起潮红的机制及其作用的消除。
J Clin Hypertens (Greenwich). 2009 Nov;11(11):685-9. doi: 10.1111/j.1559-4572.2008.00050.x.
5
Niacin: a re-emerging pharmaceutical for the treatment of dyslipidaemia.烟酸:一种用于治疗血脂异常的新兴药物。
Br J Pharmacol. 2009 Sep;158(2):429-41. doi: 10.1111/j.1476-5381.2009.00349.x. Epub 2009 Jul 20.
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FoxO1 integrates insulin signaling to VLDL production.叉头框蛋白O1(FoxO1)将胰岛素信号整合至极低密度脂蛋白(VLDL)生成过程。
Cell Cycle. 2008 Oct;7(20):3162-70. doi: 10.4161/cc.7.20.6882. Epub 2008 Oct 27.
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Flushing out the role of GPR109A (HM74A) in the clinical efficacy of nicotinic acid.阐明GPR109A(HM74A)在烟酸临床疗效中的作用。
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