نتایج جستجو برای: fxr

تعداد نتایج: 1033  

2018
Kavita Jadhav Yang Xu Yanyong Xu Yuanyuan Li Jiesi Xu Yingdong Zhu Luciano Adorini Yoon Kwang Lee Takhar Kasumov Liya Yin Yanqiao Zhang

OBJECTIVES Activation of the bile acid (BA) receptors farnesoid X receptor (FXR) or G protein-coupled bile acid receptor (GPBAR1; TGR5) improves metabolic homeostasis. In this study, we aim to determine the impact of pharmacological activation of bile acid receptors by INT-767 on reversal of diet-induced metabolic disorders, and the relative contribution of FXR vs. TGR5 to INT-767's effects on ...

Journal: :Nature communications 2013
Lihua Jin Xuhui Feng Hui Rong Zhifu Pan Yuka Inaba Lin Qiu Weili Zheng Shengchen Lin Rui Wang Zhao Wang Shanshan Wang Hongyan Liu Song Li Wen Xie Yong Li

Farnesoid X receptor (FXR) has important roles in maintaining bile acid and cholesterol homeostasis. Here we report that the antiparasitic drug ivermectin is a ligand for nuclear FXR. We identify ivermectin using a high-throughput compound library screening and show that it induces the transcriptional activity of the FXR with distinctive properties in modulating coregulator recruitment. The cry...

Journal: :FEBS letters 2010
Iuliana Ristea Popescu Audrey Helleboid-Chapman Anthony Lucas Brigitte Vandewalle Julie Dumont Emmanuel Bouchaert Bruno Derudas Julie Kerr-Conte Sandrine Caron François Pattou Bart Staels

Farnesoid X receptor (FXR) is highly expressed in liver and intestine where it controls bile acid (BA), lipid and glucose homeostasis. Here we show that FXR is expressed and functional, as assessed by target gene expression analysis, in human islets and beta-cell lines. FXR is predominantly cytosolic-localized in the islets of lean mice, but nuclear in obese mice. Compared to FXR+/+ mice, FXR-/...

Journal: :Proceedings of the National Academy of Sciences of the United States of America 2004
David Bishop-Bailey Desmond T Walsh Timothy D Warner

The farnesoid X receptor/bile acid receptor (FXR) is a recently discovered member of the nuclear hormone superfamily. FXR ligands have been proposed as targets in cardiovascular disease, regulating cholesterol metabolism and bile acid transport and metabolism in the liver and gastrointestinal tract. When we used a human cardiovascular tissue array, we found that FXR is expressed in a variety of...

Journal: :American journal of physiology. Gastrointestinal and liver physiology 2012
Hongying Su Chuang Ma Jingfeng Liu Ningbo Li Meiqin Gao Aimin Huang Xichun Wang Wendong Huang Xiongfei Huang

The nuclear receptor farnesoid X receptor (FXR) acts as a liver protector by regulating normal liver homeostasis. Spontaneously developed liver tumors have been found in FXR-null mice. However, the role of FXR in the tumorigenesis of human hepatocellular carcinoma (HCC) is still poorly understood. In this study, we measured the expression of FXR and its primary target gene, small heterodimer pa...

2012
Guodong Li Ann M. Thomas Jessica A. Williams Bo Kong Jie Liu Yuka Inaba Wen Xie Grace L. Guo

Farnesoid X receptor (FXR) is a nuclear receptor and a key regulator of liver cholesterol and triglyceride homeostasis. Scavenger receptor class B type I (SR-BI) is critical for reverse cholesterol transport (RCT) by transporting high-density lipoprotein (HDL) into liver. FXR induces SR-BI, however, the underlying molecular mechanism of this induction is not known. The current study confirmed i...

Journal: :Arteriosclerosis, thrombosis, and vascular biology 2016
Leonardo A Moraes Amanda J Unsworth Sakthivel Vaiyapuri Marfoua S Ali Parvathy Sasikumar Tanya Sage Gagan D Flora Alex P Bye Neline Kriek Emilie Dorchies Olivier Molendi-Coste David Dombrowicz Bart Staels David Bishop-Bailey Jonathan M Gibbins

OBJECTIVE Although initially seemingly paradoxical because of the lack of nucleus, platelets possess many transcription factors that regulate their function through DNA-independent mechanisms. These include the farnesoid X receptor (FXR), a member of the superfamily of ligand-activated transcription factors, that has been identified as a bile acid receptor. In this study, we show that FXR is pr...

2015
Ingrid T. G. W. Bijsmans Chiara Guercini José M. Ramos Pittol Wienand Omta Alexandra Milona Daphne Lelieveld David A. Egan Roberto Pellicciari Antimo Gioiello Saskia W. C. van Mil

The Farnesoid X receptor (FXR) regulates bile salt, glucose and cholesterol homeostasis by binding to DNA response elements, thereby activating gene expression (direct transactivation). FXR also inhibits the immune response via tethering to NF-κB (tethering transrepression). FXR activation therefore has therapeutic potential for liver and intestinal inflammatory diseases. We aim to identify and...

Journal: :Journal of lipid research 2004
Audrey Sirvent Adrie J M Verhoeven Hans Jansen Vladimir Kosykh Raphaël J Darteil Dean W Hum Jean-Charles Fruchart Bart Staels

The farnesoid X receptor (FXR) is a nuclear receptor that regulates gene expression in response to bile acids (BAs). FXR plays a central role in BA, cholesterol, and lipoprotein metabolism. Here, we identify HL, an enzyme involved in the metabolism of remnant and high density lipoproteins, as a novel FXR-regulated gene. The natural FXR ligand, chenodeoxycholic acid (CDCA), downregulates HL gene...

Journal: :The Biochemical journal 2011
Fan Lian Xiangbin Xing Gang Yuan Claus Schäfer Sandra Rauser Axel Walch Christoph Röcken Martin Ebeling Matthew B Wright Roland M Schmid Matthias P A Ebert Elke Burgermeister

Bile acids from duodenogastric reflux promote inflammation and increase the risk for gastro-oesophageal cancers. FXR (farnesoid X receptor/NR1H4) is a transcription factor regulated by bile acids such as CDCA (chenodeoxycholic acid). FXR protects the liver and the intestinal tract against bile acid overload; however, a functional role for FXR in the stomach has not been described. We detected F...

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