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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Role of farnesoid X receptor in inflammation and resolution
Firdose Begum Shaik1, Durbaka V R Prasad, Venkata Ramireddy Narala
1Department of Zoology, Yogi Vemana University, Kadapa, 516 003, AP, India.
Objective:
The aim of this paper is to review the developments of farnesoid X receptor (FXR) biology, its ligands, and various functions, in particular we discuss the anti-inflammatory and anti-fibrotic role in chronic inflammatory diseases.
Introduction:
FXR is a ligand-dependent transcription factor belonging to the nuclear hormone receptor superfamily. The accrued data have shown that the FXR plays important roles not only in bile acid, lipid metabolism, and carbohydrate homeostasis, but also in inflammatory responses. The anti-inflammatory and anti-fibrotic effects of FXR on chronic inflammatory diseases are not well documented.
Methods:
A literature survey was performed using PubMed database search to gather complete information regarding FXR and its role in inflammation.
Results And Discussion:
FXR is highly expressed in liver, intestine, kidney and adrenals, but with lower expression in fat tissue, heart and recently it has been found to express in lungs too. Primary bile acids, cholic acid and chenodeoxycholic acid are the natural endogenous ligands for FXR. GW4064 and 6α-ethyl-chenodeoxycholic acid are the synthetic high-affinity agonists. An exhaustive literature survey revealed that FXR acts as a key metabolic regulator and potential drug target for many metabolic syndromes that include chronic inflammatory diseases.
Insights
Farnesoid X receptor (FXR) is a key regulator of metabolism and inflammation. This review highlights FXR's anti-inflammatory and anti-fibrotic roles in chronic diseases, identifying it as a potential therapeutic target.
Area of Science:
- Nuclear hormone receptor superfamily
- Ligand-dependent transcription factor
Background:
- FXR regulates bile acid, lipid, and carbohydrate metabolism.
- FXR also plays a significant role in inflammatory responses.
- Its anti-inflammatory and anti-fibrotic effects in chronic diseases require further documentation.
Purpose of the Study:
- Review developments in farnesoid X receptor (FXR) biology.
- Discuss FXR ligands and functions, focusing on anti-inflammatory and anti-fibrotic roles.
- Explore FXR's potential in treating chronic inflammatory diseases.
Main Methods:
- Literature survey conducted using PubMed database.
- Focused on gathering information regarding FXR and its role in inflammation.
Main Results:
- FXR is highly expressed in the liver, intestine, kidney, and adrenals.
- Natural ligands include primary bile acids; synthetic agonists like GW4064 exist.
- FXR is a key metabolic regulator with potential as a drug target.
Conclusions:
- FXR demonstrates significant anti-inflammatory and anti-fibrotic properties.
- Its role in chronic inflammatory diseases is a promising area for therapeutic development.
- FXR represents a potential drug target for metabolic syndromes involving inflammation.
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