GPR109A and vascular inflammation.
GPR109A and vascular inflammation.
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DOI：
10.1007/s11883-013-0325-9
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发表时间：
2013-05
影响因子：
5.8
通讯作者：
Choudhury, Robin P.
中科院分区：
文献类型：
--
作者：
Chai, Joshua T.;Digby, Janet E.;Choudhury, Robin P.
关键词：
自从十年前发现GPR 109 A作为烟酸的受体，沿着不久后作为内源性配体3-羟基丁酸的受体去乙酰化以来，GPR 109 A引起了广泛的兴趣。这种兴趣的产生，特别是因为烟酸的“多效性”的作用机制和其在代谢和炎症途径之间的“串扰”的潜力的持续探索。作为GPR 109 A在临床应用中的主要药理学配体，烟酸已用于治疗心血管疾病超过50年，主要是由于其对血浆脂蛋白的有利作用。然而，很明显，烟酸也具有脂蛋白非依赖性作用，影响通过GPR 109 A介导的炎症途径。除了G蛋白介导的作用外，最近的证据也支持GPR 109 A通过适应性蛋白β-抑制蛋白进行信号传导。在这篇文章中，我们认为GPR 109 A的作用及其下游效应的背景下，动脉粥样硬化和血管炎症，沿着洞察未来的药物开发策略。
GPR109A has generated expanding interest since its discovery as the receptor for niacin a decade ago, along with deorphanisation as the receptor for endogenous ligand 3-hydroxy-butyrate shortly after. This interest is generated especially because of the continuing exploration of niacin’s “pleiotropic” mechanisms of action and its potential in the “cross-talk” between metabolic and inflammatory pathways. As GPR109A’s primary pharmacological ligand in clinical use, niacin has been used for over 50 years in the treatment of cardiovascular disease, mainly due to its favourable effects on plasma lipoproteins. However, it has become apparent that niacin also possesses lipoprotein-independent effects that influence inflammatory pathways mediated through GPR109A. In addition to its G-protein–mediated effects, recent evidence has emerged to support alternative GPR109A signalling via adaptive protein β-arrestins. In this article, we consider the role of GPR109A and its downstream effects in the context of atherosclerosis and vascular inflammation, along with insights into strategy for future drug development.
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影响因子：
5.3
作者：
Ganji, Shobha H.;Qin, Shucun;Kashyap, Moti L.
通讯作者：
Kashyap, Moti L.
DOI：
10.1006/bbrc.1997.7236
发表时间：
1997-09-08
影响因子：
3.1
作者：
Calabresi, L;Franceschini, G;Taramelli, D
通讯作者：
Taramelli, D
DOI：
10.1161/atvbaha.111.241836
发表时间：
2012-03
期刊：
Arteriosclerosis, thrombosis, and vascular biology
影响因子：
--
作者：
Digby JE;Martinez F;Jefferson A;Ruparelia N;Chai J;Wamil M;Greaves DR;Choudhury RP
通讯作者：
Choudhury RP
DOI：
10.1161/01.atv.15.11.1987
发表时间：
1995-11-01
影响因子：
8.7
作者：
COCKERILL, GW;RYE, KA;BARTER, PJ
通讯作者：
BARTER, PJ
影响因子：
82.9
作者：
Chinetti, G;Lestavel, S;Staels, B
通讯作者：
Staels, B