Abstract
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.Keywords: FXR, atherosclerosis, agonist, bile acids, pharmaceutical target, clinical trials.
Current Medicinal Chemistry
Title:Farnesoid-X Receptor (FXR) as a Promising Pharmaceutical Target in Atherosclerosis
Volume: 24 Issue: 11
Author(s): Demetrios Moris, Constantinos Giaginis*, Gerasimos Tsourouflis and Stamatios Theocharis
Affiliation:
- Department of Food Science and Nutrition, University of the Aegean, 2 Mitropoliti Ioakeim Street, Myrina, Lemnos 81400,Greece
Keywords: FXR, atherosclerosis, agonist, bile acids, pharmaceutical target, clinical trials.
Abstract: 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
About this article
Cite this article as:
Moris Demetrios, Giaginis Constantinos*, Tsourouflis Gerasimos and Theocharis Stamatios, 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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