Document Detail

Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease.
MedLine Citation:
PMID:  22550135     Owner:  NLM     Status:  MEDLINE    
Dyslipidemia is an important risk factor for cardiovascular disease (CVD) and atherosclerosis. When dyslipidemia coincides with other metabolic disorders such as obesity, hypertension, and glucose intolerance, defined as the metabolic syndrome (MS), individuals present an elevated risk to develop type 2 diabetes (T2D) as well as CVD. Because the MS epidemic represents a growing public health problem worldwide, the development of therapies remains a major challenge. Alterations of bile acid pool regulation in T2D have revealed a link between bile acid and metabolic homeostasis. The bile acid receptors farnesoid X receptor (FXR) and TGR5 both regulate lipid, glucose, and energy metabolism, rendering them potential pharmacological targets for MS therapy. This review discusses the mechanisms of metabolic regulation by FXR and TGR5 and the utility relevance of natural and synthetic modulators of FXR and TGR5 activity, including bile acid sequestrants, in the treatment of the MS.
Geoffrey Porez; Janne Prawitt; Barbara Gross; Bart Staels
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2012-05-01
Journal Detail:
Title:  Journal of lipid research     Volume:  53     ISSN:  0022-2275     ISO Abbreviation:  J. Lipid Res.     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-08-08     Completed Date:  2012-12-06     Revised Date:  2013-09-03    
Medline Journal Info:
Nlm Unique ID:  0376606     Medline TA:  J Lipid Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1723-37     Citation Subset:  IM    
Université Lille Nord de France, F-59000 Lille, France.
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MeSH Terms
Bile Acids and Salts / metabolism*
Cardiovascular Diseases / drug therapy*,  metabolism
Dyslipidemias / drug therapy*,  metabolism
Molecular Targeted Therapy / methods*
Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors,  metabolism*
Receptors, G-Protein-Coupled / agonists,  metabolism*
Reg. No./Substance:
0/Bile Acids and Salts; 0/GPBAR1 protein, human; 0/Receptors, Cytoplasmic and Nuclear; 0/Receptors, G-Protein-Coupled; 0/farnesoid X-activated receptor

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