Farnesoid X receptor (FXR): Structures and ligands

[Display omitted] Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in t...

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Bibliographic Details
Published in:Computational and structural biotechnology journal Vol. 19; pp. 2148 - 2159
Main Authors: Jiang, Longying, Zhang, Huajun, Xiao, Desheng, Wei, Hudie, Chen, Yongheng
Format: Journal Article
Language:English
Published: Netherlands Elsevier B.V 01.01.2021
Research Network of Computational and Structural Biotechnology
Elsevier
Subjects:
Agonists
Antagonists
bile
bile acids
biotechnology
domain
drugs
Farnesoid X receptor
intestines
Ligand binding domain
ligands
liver
metabolism
resorption
Review
Structure
therapeutics
Farnesoid X receptor
Agonists
Antagonists
Structure
Ligand binding domain
ISSN:2001-0370, 2001-0370
Online Access:Get full text
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Summary:[Display omitted] Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.
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ISSN:2001-0370
2001-0370
DOI:10.1016/j.csbj.2021.04.029