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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Vydáno v:Computational and structural biotechnology journal Ročník 19; s. 2148 - 2159
Hlavní autoři: Jiang, Longying, Zhang, Huajun, Xiao, Desheng, Wei, Hudie, Chen, Yongheng
Médium: Journal Article
Jazyk:angličtina
Vydáno: Netherlands Elsevier B.V 01.01.2021
Research Network of Computational and Structural Biotechnology
Elsevier
Témata:
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
On-line přístup:Získat plný text
Tagy: Přidat tag
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Abstract [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.
AbstractList [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.
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.
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.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.
Author Jiang, Longying
Xiao, Desheng
Chen, Yongheng
Zhang, Huajun
Wei, Hudie
Author_xml – sequence: 1
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  surname: Jiang
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  surname: Xiao
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  organization: Department of Pathology, NHC Key Laboratory of Cancer Proteomics, Laboratory of Structural Biology, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China
– sequence: 4
  givenname: Hudie
  surname: Wei
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  surname: Chen
  fullname: Chen, Yongheng
  email: yonghenc@163.com
  organization: Department of Pathology, NHC Key Laboratory of Cancer Proteomics, Laboratory of Structural Biology, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China
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Keywords Farnesoid X receptor
Agonists
Antagonists
Structure
Ligand binding domain
Language English
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  year: 2021
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PublicationTitle Computational and structural biotechnology journal
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Elsevier
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Snippet [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...
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...
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SubjectTerms Agonists
Antagonists
bile
bile acids
biotechnology
domain
drugs
Farnesoid X receptor
intestines
Ligand binding domain
ligands
liver
metabolism
resorption
Review
Structure
therapeutics
Title Farnesoid X receptor (FXR): Structures and ligands
URI https://dx.doi.org/10.1016/j.csbj.2021.04.029
https://www.ncbi.nlm.nih.gov/pubmed/33995909
https://www.proquest.com/docview/2528432525
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