摘要
背景:动脉粥样硬化(AS)是西方世界的死亡和致残的主要原因,是与致动脉粥样化脂蛋白和炎症密切相关。胆汁酸(BA)作为激活内源性配体如法尼基-X受体(FXR)信号。初步数据表明FXR的潜在作用,但FXR配体在AS中的治疗价值是未知的。 目的:本综述,分析了FXR激动剂作为一种治疗方式的疗效对。在这方面,我们进行电子搜索通过Pub- Med/MEDLINE数据库使用的关键术语:受体,动脉粥样硬化,胆汁酸和激动 。 结论:根据我们的分析,FXR似乎是动脉粥样硬化自然史上有希望的治疗靶点。FXR激动可以在AS的发展和发展中发挥保护作用。 然而,FXR激动存在已经报道的副作用,例如血浆HDL的降低。最后,使用合成FXR激动剂进行临床试验的结果将更多地反映FXR激动在AS治疗中的确切作用。
关键词: FXR,动脉粥样硬化,激动剂,胆汁酸,药物靶标,临床试验。
Current Medicinal Chemistry
Title:Farnesoid-X Receptor (FXR) as a Promising Pharmaceutical Target in Atherosclerosis
Volume: 24 Issue: 11
关键词: FXR,动脉粥样硬化,激动剂,胆汁酸,药物靶标,临床试验。
摘要: Background: Atherosclerosis (AS) is a major cause of death and morbidity in Western world and is strongly connected with atherogenic lipoproteins and inflammation. Bile acids (BA) act as activating signals of endogenous ligands such as Farnesoid-X receptor (FXR). Primary data indicate a potential role of FXR in AS. The therapeutic value of FXR ligands in AS is unknown.
Objective: With the present review, we analyzed the efficacy of FXR agonists as a therapeutic modalities against AS. In this aspect, we performed an electronic search through Pub- Med/MEDLINE database by using the key terms: FXR*, Farnesoid X receptor*, atherosclerosis*, bile acids* and agonism*. Conclusion: According to our analysis, the FXR seems to be a promising therapeutic target in the atherosclerosis natural history. FXR agonism could exert protective effects in the development and evolution of AS. However, concomitant side effects such as the reduction of plasma HDL have been reported. Finally, results from undergoing clinical trials with synthetic FXR agonists will shed more light to the precise role of FXR agonism in AS treatment.Export Options
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Cite this article as:
Farnesoid-X Receptor (FXR) as a Promising Pharmaceutical Target in Atherosclerosis, Current Medicinal Chemistry 2017; 24 (11) . https://dx.doi.org/10.2174/0929867324666170124151940
DOI https://dx.doi.org/10.2174/0929867324666170124151940 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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