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Epigenetic regulation and posttranslational modifications of FXR: underlying mechanisms and implications in digestive
Qian-Rui Mi1, Cai-Qian Wu1, Cheng-Guo Lv1
1Zhongnan Hospital of Wuhan University, Institute of Hepatobiliary Diseases of Wuhan University, Transplant Center of Wuhan University, National Quality Control Center for Donated Organ Procurement, Hubei Key Laboratory of Medical Technology on Transplantation, Wuhan, 430071, China.
Abstract:
The incidence of digestive system diseases is increasing, with liver diseases, obesity, inflammatory bowel disease (IBD), and hepatoenteric cancers being prominent contributors to global morbidity and mortality. Targeting farnesoid X receptor (FXR) has emerged as a promising therapeutic strategy for various digestive disorders. FXR is a member of the nuclear receptor superfamily, is expressed primarily in the liver and small intestine, and is activated by bile acids (BAs). Beyond classical ligand-dependent activation, FXR activity is precisely modulated by epigenetic regulation and posttranslational modifications (PTMs), such as DNA methylation, histone methylation and acetylation, noncoding RNA regulation, phosphorylation, acetylation, SUMOylation, ubiquitination, O-glycosylation, methylation, sulfhydration, and poly(ADP-ribosyl)ation. Growing evidence reveals disease-associated alterations in FXR modification patterns, offering novel therapeutic perspectives for digestive pathologies. In this review, we comprehensively summarize the structure of FXR, its regulatory mechanisms through epigenetic modifications and PTMs, and its potential application in the treatment of digestive diseases. The structure of FXR, its regulatory mechanisms through epigenetic modifications and PTMs, and its potential application in the treatment of digestive diseases. Upper: epigenetic regulation of FXR. Below: posttranslational modifications of FXR. OG O-glycosylation, P phosphorylation, SUMO SUMOylation, SSH sulfhydration, Ac acetylation, Me methylation, Ub ubiquitination.
Insights
Targeting the farnesoid X receptor (FXR) offers new therapeutic avenues for digestive diseases. Understanding its epigenetic and posttranslational modifications is key to developing effective treatments for liver diseases and IBD.
Area of Science:
- Gastroenterology and Hepatology
- Molecular Biology
- Pharmacology
Background:
- Digestive system diseases, including liver diseases, obesity, inflammatory bowel disease (IBD), and hepatoenteric cancers, represent a growing global health burden.
- The farnesoid X receptor (FXR), a nuclear receptor activated by bile acids, is a key regulator in the liver and small intestine.
- Dysregulation of FXR is implicated in the pathogenesis of various digestive disorders.
Purpose of the Study:
- To comprehensively review the structure and regulatory mechanisms of FXR.
- To explore the role of epigenetic modifications and posttranslational modifications (PTMs) in FXR activity.
- To discuss the therapeutic potential of targeting FXR for digestive diseases.
Main Methods:
- Literature review synthesizing current research on FXR.
- Analysis of epigenetic modifications (e.g., DNA methylation, histone modifications, noncoding RNA regulation) affecting FXR.
- Examination of various posttranslational modifications (PTMs) of FXR, including phosphorylation, acetylation, SUMOylation, ubiquitination, O-glycosylation, methylation, sulfhydration, and poly(ADP-ribosyl)ation.
Main Results:
- FXR activity is modulated by a complex interplay of ligand-dependent activation, epigenetic regulation, and PTMs.
- Altered FXR modification patterns are associated with the development of digestive pathologies.
- Specific PTMs and epigenetic changes offer potential therapeutic targets.
Conclusions:
- FXR represents a promising therapeutic target for a range of digestive diseases.
- Further research into FXR's regulatory network, including epigenetic and PTMs, is crucial for developing novel treatments.
- Understanding these modifications can lead to targeted therapies for liver diseases, IBD, and related cancers.
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