ファルネソイドX受容体 farnesoid X receptor

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the 6th letter of the Roman alphabet (同)f

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/11/06 14:47:40」(JST)

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English Journal

Activation of farnesoid X receptor induces RECK expression in mouse liver.

Peng X1, Wu W2, Zhu B1, Sun Z1, Ji L1, Ruan Y1, Zhou M3, Zhou L4, Gu J2.Author information 1Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China.2Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China; Institutes of Biomedical Sciences, Fudan University, Shanghai 200032, China.3Department of Radiology, Zhongshan Hospital of Fudan University and Shanghai Institute of Medical Imaging, Shanghai 200032, China. Electronic address: meilingzhou2012@gmail.com.4Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China. Electronic address: yhchloech@gmail.com.AbstractFarnesoid X receptor (FXR) belongs to the ligand-activated nuclear receptor superfamily, and functions as a transcription factor regulating the transcription of numerous genes involved in bile acid homeostasis, lipoprotein and glucose metabolism. In the present study, we identified RECK, a membrane-anchored inhibitor of matrix metalloproteinases, as a novel target gene of FXR in mouse liver. We found that FXR agonist substantially augmented hepatic RECK mRNA and protein expression in vivo and in vitro. FXR regulated the transcription of RECK through directly binding to FXR response element located within intron 1 of the mouse RECK gene. Moreover, FXR agonist reversed the down-regulation of RECK in the livers from mice fed a methionine and choline deficient diet. In summary, our data suggest that RECK is a novel transcriptional target of FXR in mouse liver, and provide clues to better understanding the function of FXR in liver.
Biochemical and biophysical research communications.Biochem Biophys Res Commun.2014 Jan 3;443(1):211-6. doi: 10.1016/j.bbrc.2013.11.082. Epub 2013 Nov 28.
Farnesoid X receptor (FXR) belongs to the ligand-activated nuclear receptor superfamily, and functions as a transcription factor regulating the transcription of numerous genes involved in bile acid homeostasis, lipoprotein and glucose metabolism. In the present study, we identified RECK, a membrane-
PMID 24291500

Activation of farnesoid X receptor attenuates hepatic injury in a murine model of alcoholic liver disease.

Wu W1, Zhu B2, Peng X2, Zhou M3, Jia D4, Gu J1.Author information 1Department of Biochemistry and Molecular Biology, Shanghai Medical College, Fudan University, Shanghai 200032, China; Institutes of Biomedical Science, Fudan University, Shanghai 200032, China.2Department of Biochemistry and Molecular Biology, Shanghai Medical College, Fudan University, Shanghai 200032, China.3Department of Radiology, Zhongshan Hospital of Fudan University and Shanghai Institute of Medical Imaging, Shanghai 200032, China. Electronic address: meilingzhou2012@gmail.com.4Department of Biochemistry and Molecular Biology, Shanghai Medical College, Fudan University, Shanghai 200032, China. Electronic address: jiadongwei@fudan.edu.cn.AbstractAlcoholic liver disease (ALD) is a common cause of advanced liver disease, and considered as a major risk factor of morbidity and mortality worldwide. Hepatic cholestasis is a pathophysiological feature observed in all stages of ALD. The farnesoid X receptor (FXR) is a member of the nuclear hormone receptor superfamily, and plays an essential role in the regulation of bile acid, lipid and glucose homeostasis. However, the role of FXR in the pathogenesis and progression of ALD remains largely unknown. Mice were fed Lieber-DeCarli ethanol diet or an isocaloric control diet. We used a specific agonist of FXR WAY-362450 to study the effect of pharmacological activation of FXR in alcoholic liver disease. In this study, we demonstrated that FXR activity was impaired by chronic ethanol ingestion in a murine model of ALD. Activation of FXR by specific agonist WAY-362450 protected mice from the development of ALD. We also found that WAY-362450 treatment rescued FXR activity, suppressed ethanol-induced Cyp2e1 up-regulation and attenuated oxidative stress in liver. Our results highlight a key role of FXR in the modulation of ALD development, and propose specific FXR agonists for the treatment of ALD patients.
Biochemical and biophysical research communications.Biochem Biophys Res Commun.2014 Jan 3;443(1):68-73. doi: 10.1016/j.bbrc.2013.11.057. Epub 2013 Nov 20.
Alcoholic liver disease (ALD) is a common cause of advanced liver disease, and considered as a major risk factor of morbidity and mortality worldwide. Hepatic cholestasis is a pathophysiological feature observed in all stages of ALD. The farnesoid X receptor (FXR) is a member of the nuclear hormone
PMID 24269813

Characterizing ligands for farnesoid X receptor - available in vitro test systems for farnesoid X receptor modulator development.

Merk D, Steinhilber D, Schubert-Zsilavecz M.Author information Goethe-University Frankfurt, Institute of Pharmaceutical Chemistry , Max-von-Laue-Str. 9, D-60438 Frankfurt am Main , Germany merk@pharmchem.uni-frankfurt.de.AbstractIntroduction: Farnesoid X receptor (FXR) is an ascending target for metabolic and inflammatory diseases. As a nuclear receptor, FXR exhibits many physiological effects in transcription control of several genes. Therefore, the development of synthetic FXR ligands requires elaborate in vitro test systems to characterize novel ligands and to estimate their in vivo activities. Areas covered: This work gathers and describes published in vitro test systems for FXR ligands including cell-based functional assays as well as binding assays. It also evaluates the information which can be provided by these assays. Expert opinion: In vitro screening of FXR ligands widely relies on reporter gene assays. Additionally, some co-activator re-cruitment assays are described and for the characterization of potent compounds the pattern of affected target genes is evaluated by qPCR. Compared to other nuclear receptors such as PPARs the variety of test systems is quite low for FXR and might eventually not be enough to sufficiently characterize FXR targeting drug candidates.
Expert opinion on drug discovery.Expert Opin Drug Discov.2014 Jan;9(1):27-37. doi: 10.1517/17460441.2014.860129. Epub 2013 Nov 21.
Introduction: Farnesoid X receptor (FXR) is an ascending target for metabolic and inflammatory diseases. As a nuclear receptor, FXR exhibits many physiological effects in transcription control of several genes. Therefore, the development of synthetic FXR ligands requires elaborate in vitro test syst
PMID 24261510

Japanese Journal

Consumption of Soy Protein Isolate Reduces Hepatic SREBP-1c and Lipogenic Gene Expression in Wild-Type Mice, but Not in FXR-Deficient Mice

HASHIDUME Tsutomu,SASAKI Takashi,INOUE Jun,SATO Ryuichiro
Bioscience, biotechnology, and biochemistry 75(9), 1702-1707, 2011-09-23
… We also examined SPI-mediated effects in farnesoid X receptor (FXR)-deficient mice. … No effects of SPI were observed in the FXR-deficient mice, suggesting the importance of FXR. … Hepatic peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α) gene expression was reduced by SPI, and this might be associated with a decrease in FXR expression. …
NAID 10029756995

Effect of Peucedanum japonicum Thunb on the Expression of Obesity-Related Genes in Mice on a High-Fat Diet

Nukitrangsan Natthanan,Okabe Takafumi,Toda Takayoshi,Inafuku Masashi,Iwasaki Hironori,Yanagita Teruyoshi,Oku Hirosuke
Journal of Oleo Science 60(10), 527-536, 2011
… PJT increased the expression of PPARγ, FXRα, DGAT1, and ATGL genes, suggesting an enhancement of adipocyte differentiation and normalization of functionality of adipose tissue. …
NAID 130001008506