Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?

Salvatore Modica; Antonio Moschetta

doi:10.1016/j.febslet.2006.07.082

Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?

Salvatore Modica, Antonio Moschetta

Pharmacology

Research output: Contribution to journal › Short survey › peer-review

78 Scopus citations

Abstract

The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.

Original language	English (US)
Pages (from-to)	5492-5499
Number of pages	8
Journal	FEBS Letters
Volume	580
Issue number	23
DOIs	https://doi.org/10.1016/j.febslet.2006.07.082
State	Published - Oct 9 2006

Keywords

Cholesterol
Farnesoid X receptor
Gallstones
Hypertriglyceridemia
Metabolic syndrome

ASJC Scopus subject areas

Biophysics
Structural Biology
Biochemistry
Molecular Biology
Genetics
Cell Biology

Access to Document

10.1016/j.febslet.2006.07.082

Cite this

@article{c1206d44b16948b799c3dfd3fadaddf0,

title = "Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?",

abstract = "The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.",

keywords = "Cholesterol, Farnesoid X receptor, Gallstones, Hypertriglyceridemia, Metabolic syndrome",

author = "Salvatore Modica and Antonio Moschetta",

note = "Funding Information: This work was partly supported by Italian Association for Cancer Research (AIRC), Italian Ministero dell{\textquoteright}Universit{\`a} e della Ricerca Scientifica, Fondazione NegriSud and University of Bari, Italy. We thank all the members of the laboratory for critically reading the manuscript. We apologize to our distinguished colleagues that many primary references could not be included because of space limitation.",

year = "2006",

month = oct,

day = "9",

doi = "10.1016/j.febslet.2006.07.082",

language = "English (US)",

volume = "580",

pages = "5492--5499",

journal = "FEBS Letters",

issn = "0014-5793",

publisher = "Elsevier",

number = "23",

}

TY - JOUR

T1 - Nuclear bile acid receptor FXR as pharmacological target

T2 - Are we there yet?

AU - Modica, Salvatore

AU - Moschetta, Antonio

N1 - Funding Information: This work was partly supported by Italian Association for Cancer Research (AIRC), Italian Ministero dell’Università e della Ricerca Scientifica, Fondazione NegriSud and University of Bari, Italy. We thank all the members of the laboratory for critically reading the manuscript. We apologize to our distinguished colleagues that many primary references could not be included because of space limitation.

PY - 2006/10/9

Y1 - 2006/10/9

N2 - The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.

AB - The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is primarily expressed in the enterohepatic system where it functions as intracellular sensor for bile acids. Ligand dependent FXR activation induces transcriptional responses to coordinately regulate bile acid, cholesterol, triglyceride and glucose metabolism, and to protect the intestinal mucosa from bacterial overgrowth and inflammatory insults. Here we discuss the latest discoveries in FXR-driven metabolic pathways with relevance to pathophysiology and novel therapeutic approaches of several conditions such as hypertriglyceridemia, type 2 diabetes, cholesterol gallstone disease, steato-hepatitis and metabolic syndrome.

KW - Cholesterol

KW - Farnesoid X receptor

KW - Gallstones

KW - Hypertriglyceridemia

KW - Metabolic syndrome

UR - http://www.scopus.com/inward/record.url?scp=33749344968&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33749344968&partnerID=8YFLogxK

U2 - 10.1016/j.febslet.2006.07.082

DO - 10.1016/j.febslet.2006.07.082

M3 - Short survey

C2 - 16904670

AN - SCOPUS:33749344968

SN - 0014-5793

VL - 580

SP - 5492

EP - 5499

JO - FEBS Letters

JF - FEBS Letters

IS - 23

ER -

Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this