The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity
The nuclear receptor farnesoid X receptor (FXR, NR1H4) is a bile acid (BA) sensor that links the enterohepatic circuit that regulates BA metabolism and elimination to systemic lipid homeostasis. Furthermore, FXR represents a real guardian of the hepatic function, preserving, in a multifactorial fash...
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-11-01
|
| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/23/22/13967 |
| _version_ | 1797465123773743104 |
|---|---|
| author | Magdalena Rausch Sophia L. Samodelov Michele Visentin Gerd A. Kullak-Ublick |
| author_facet | Magdalena Rausch Sophia L. Samodelov Michele Visentin Gerd A. Kullak-Ublick |
| author_sort | Magdalena Rausch |
| collection | DOAJ |
| description | The nuclear receptor farnesoid X receptor (FXR, NR1H4) is a bile acid (BA) sensor that links the enterohepatic circuit that regulates BA metabolism and elimination to systemic lipid homeostasis. Furthermore, FXR represents a real guardian of the hepatic function, preserving, in a multifactorial fashion, the integrity and function of hepatocytes from chronic and acute insults. This review summarizes how FXR modulates the expression of pathway-specific as well as polyspecific transporters and enzymes, thereby acting at the interface of BA, lipid and drug metabolism, and influencing the onset and progression of hepatotoxicity of varying etiopathogeneses. Furthermore, this review article provides an overview of the advances and the clinical development of FXR agonists in the treatment of liver diseases. |
| first_indexed | 2024-03-09T18:18:01Z |
| format | Article |
| id | doaj.art-c398b3201b114988baf3d2f4fb5d4ff0 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-09T18:18:01Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-c398b3201b114988baf3d2f4fb5d4ff02023-11-24T08:36:22ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-11-0123221396710.3390/ijms232213967The Farnesoid X Receptor as a Master Regulator of HepatotoxicityMagdalena Rausch0Sophia L. Samodelov1Michele Visentin2Gerd A. Kullak-Ublick3Department of Clinical Pharmacology and Toxicology, University Hospital Zurich, University of Zurich, 8006 Zurich, SwitzerlandDepartment of Clinical Pharmacology and Toxicology, University Hospital Zurich, University of Zurich, 8006 Zurich, SwitzerlandDepartment of Clinical Pharmacology and Toxicology, University Hospital Zurich, University of Zurich, 8006 Zurich, SwitzerlandDepartment of Clinical Pharmacology and Toxicology, University Hospital Zurich, University of Zurich, 8006 Zurich, SwitzerlandThe nuclear receptor farnesoid X receptor (FXR, NR1H4) is a bile acid (BA) sensor that links the enterohepatic circuit that regulates BA metabolism and elimination to systemic lipid homeostasis. Furthermore, FXR represents a real guardian of the hepatic function, preserving, in a multifactorial fashion, the integrity and function of hepatocytes from chronic and acute insults. This review summarizes how FXR modulates the expression of pathway-specific as well as polyspecific transporters and enzymes, thereby acting at the interface of BA, lipid and drug metabolism, and influencing the onset and progression of hepatotoxicity of varying etiopathogeneses. Furthermore, this review article provides an overview of the advances and the clinical development of FXR agonists in the treatment of liver diseases.https://www.mdpi.com/1422-0067/23/22/13967drug-induced liver injuryfarnesoid X receptor (FXR)hepatotoxicityinflammationliverNAFLD and NASH |
| spellingShingle | Magdalena Rausch Sophia L. Samodelov Michele Visentin Gerd A. Kullak-Ublick The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity International Journal of Molecular Sciences drug-induced liver injury farnesoid X receptor (FXR) hepatotoxicity inflammation liver NAFLD and NASH |
| title | The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity |
| title_full | The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity |
| title_fullStr | The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity |
| title_full_unstemmed | The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity |
| title_short | The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity |
| title_sort | farnesoid x receptor as a master regulator of hepatotoxicity |
| topic | drug-induced liver injury farnesoid X receptor (FXR) hepatotoxicity inflammation liver NAFLD and NASH |
| url | https://www.mdpi.com/1422-0067/23/22/13967 |
| work_keys_str_mv | AT magdalenarausch thefarnesoidxreceptorasamasterregulatorofhepatotoxicity AT sophialsamodelov thefarnesoidxreceptorasamasterregulatorofhepatotoxicity AT michelevisentin thefarnesoidxreceptorasamasterregulatorofhepatotoxicity AT gerdakullakublick thefarnesoidxreceptorasamasterregulatorofhepatotoxicity AT magdalenarausch farnesoidxreceptorasamasterregulatorofhepatotoxicity AT sophialsamodelov farnesoidxreceptorasamasterregulatorofhepatotoxicity AT michelevisentin farnesoidxreceptorasamasterregulatorofhepatotoxicity AT gerdakullakublick farnesoidxreceptorasamasterregulatorofhepatotoxicity |