Document Detail

Deciphering the nuclear bile acid receptor FXR paradigm.
MedLine Citation:
PMID:  21383957     Owner:  NLM     Status:  MEDLINE    
Originally called retinoid X receptor interacting protein 14 (RIP14), the farnesoid X receptor (FXR) was renamed after the ability of its rat form to bind supra-physiological concentrations of farnesol. In 1999 FXR was de-orphanized since primary bile acids were identified as natural ligands. Strongly expressed in the liver and intestine, FXR has been shown to be the master transcriptional regulator of several entero-hepatic metabolic pathways with relevance to the pathophysiology of conditions such as cholestasis, fatty liver disease, cholesterol gallstone disease, intestinal inflammation and tumors. Furthermore, given the importance of FXR in the gut-liver axis feedbacks regulating lipid and glucose homeostasis, FXR modulation appears to have great input in diseases such as metabolic syndrome and diabetes. Exciting results from several cellular and animal models have provided the impetus to develop synthetic FXR ligands as novel pharmacological agents. Fourteen years from its discovery, FXR has gone from bench to bedside; a novel nuclear receptor ligand is going into clinical use.
Salvatore Modica; Raffaella M Gadaleta; Antonio Moschetta
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2010-11-19
Journal Detail:
Title:  Nuclear receptor signaling     Volume:  8     ISSN:  1550-7629     ISO Abbreviation:  Nucl Recept Signal     Publication Date:  2010  
Date Detail:
Created Date:  2011-03-08     Completed Date:  2011-06-14     Revised Date:  2013-06-30    
Medline Journal Info:
Nlm Unique ID:  101237902     Medline TA:  Nucl Recept Signal     Country:  United States    
Other Details:
Languages:  eng     Pagination:  e005     Citation Subset:  IM    
Laboratory of Lipid Metabolism and Cancer, Consorzio Mario Negri Sud, Santa Maria Imbaro, Chieti, Italy.
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MeSH Terms
Atherosclerosis / drug therapy
Bile Acids and Salts / chemistry*,  genetics,  metabolism
Cholestasis / drug therapy,  metabolism
Diabetes Mellitus / drug therapy
Gallstones / drug therapy,  metabolism
Gastrointestinal Stromal Tumors / drug therapy,  metabolism
Gene Expression Regulation / genetics
Glucose / metabolism
Hyperlipidemias / drug therapy
Intestinal Diseases / drug therapy,  metabolism
Liver Neoplasms / drug therapy,  metabolism
Liver Regeneration
Receptors, Cytoplasmic and Nuclear / biosynthesis,  chemistry*,  genetics,  metabolism,  therapeutic use*
Transcription Factors / genetics,  metabolism,  physiology
Triglycerides / metabolism
Reg. No./Substance:
0/Bile Acids and Salts; 0/Receptors, Cytoplasmic and Nuclear; 0/Transcription Factors; 0/Triglycerides; 0/farnesoid X-activated receptor; 50-99-7/Glucose

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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