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关键词:'G5172'
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Lihua Jin et al.
Scientific reports, 5, 17288-17288 (2015-12-02)
Non-alcoholic fatty liver disease (NAFLD) has become a predictive factor of death from many diseases. Farnesoid X receptor (FXR) is an ideal target for NAFLD drug development due to its crucial roles in lipid metabolism. The aim of this work
Faten A Al-Aqil et al.
Biochimica et biophysica acta. Molecular basis of disease, 1864(9 Pt B), 2927-2937 (2018-06-09)
At high doses, glucocorticoids (GC) have been associated with enhanced serum bile acids and liver injury. We have evaluated the effect of GC, in the absence of hepatotoxicity, on FXR/FGF91(Fgf15)/FGF21-mediated ileum-liver crosstalk. Rats and mice (wild type and Fxr-/-, Fgf15-/-
Cinzia Giordano et al.
Scientific reports, 6, 21782-21782 (2016-02-24)
Cancer-associated fibroblasts (CAFs), the principal components of the tumor stroma, play a central role in cancer development and progression. As an important regulator of the crosstalk between breast cancer cells and CAFs, the cytokine leptin has been associated to breast
Mingyi Liu et al.
Frontiers in pharmacology, 11, 375-375 (2020-04-16)
Berberine, a quinoline alkaloid, can be used in combination with statins to enhance hypolipidemic effects and reduce the dose and side effects of statins. The hypolipidemic effects of statins in the liver are mainly regulated by organic anion transporting polypeptides
Hailiang Liu et al.
Journal of lipid research, 57(10), 1831-1844 (2016-08-19)
Cholesterol 7α-hydroxylase (CYP7A1) plays a critical role in control of bile acid and cholesterol homeostasis. Bile acids activate farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5) to regulate lipid, glucose, and energy metabolism. However, the role of
Rebekka Pohl et al.
European journal of clinical investigation, 47(1), 7-18 (2016-11-01)
Chemerin is associated with insulin resistance and is expressed in the liver. Nonalcoholic fatty liver disease (NAFLD) is related to impaired insulin sensitivity, but studies evaluating hepatic and serum chemerin in NAFLD resulted in discordant data. Chemerin mRNA was determined
Chunfeng Lu et al.
IUBMB life, 67(8), 645-658 (2015-08-26)
Alcoholic liver disease (ALD) is a common health problem worldwide, characterized by aberrant accumulation of lipid in hepatocytes. Inhibition of lipid accumulation has been well recognized as a promising strategy for ALD. Previous studies showed that curcumin has potential effect
Woo-Cheol Sim et al.
The Journal of pharmacology and experimental therapeutics, 355(3), 362-369 (2015-09-20)
Liver X receptor (LXR) is a member of the nuclear receptor superfamily, and it regulates various biologic processes, including de novo lipogenesis, cholesterol metabolism, and inflammation. Selective inhibition of LXR may aid the treatment of nonalcoholic fatty liver diseases. In
Elizabeth J Tarling et al.
The Journal of clinical investigation, 127(10), 3741-3754 (2017-09-12)
Bile acids function not only as detergents that facilitate lipid absorption but also as signaling molecules that activate the nuclear receptor farnesoid X receptor (FXR). FXR agonists are currently being evaluated as therapeutic agents for a number of hepatic diseases
Mei-Fei Yueh et al.
Proceedings of the National Academy of Sciences of the United States of America, 111(48), 17200-17205 (2014-11-19)
Triclosan [5-chloro-2-(2,4-dichlorophenoxy)phenol; TCS] is a synthetic, broad-spectrum antibacterial chemical used in a wide range of consumer products including soaps, cosmetics, therapeutics, and plastics. The general population is exposed to TCS because of its prevalence in a variety of daily care
Ming Gu et al.
British journal of pharmacology, 174(18), 3032-3044 (2017-06-25)
Morin is a natural occurring flavonoid in many dietary plants and has a wide range of beneficial effects on metabolism; however, the mechanism underlying its action remains elusive. A reporter assay and the time-resolved FRET assay were used to identify
Meijing Liu et al.
Antioxidants & redox signaling, 33(2), 87-116 (2020-02-11)
Aims: Acetaminophen (APAP) overdose leads to acute liver injury by inducing hepatic mitochondrial oxidative stress and inflammation. However, the
Xin Xu et al.
Metabolism: clinical and experimental, 85, 126-138 (2018-03-27)
Farnesoid X receptor (FXR) as a member of nuclear receptor is tightly associated with glucose metabolism. Accumulated evidence has addressed the potential of FXR antagonist in the treatment of type 2 diabetes mellitus (T2DM), although the related mechanisms remain unclear.
Xiaoying Liu et al.
Hepatology (Baltimore, Md.), 68(1), 304-316 (2018-01-30)
Bile acids are endogenous ligands of the nuclear receptor, farnesoid X receptor (FXR), and pharmacological FXR modulators are under development for the treatment of several liver disorders. The inositol-requiring enzyme 1α/X-box binding protein 1 (IRE1α/XBP1) pathway of the unfolded protein
Jinxin Liu et al.
Pharmacological research, 152, 104631-104631 (2020-01-09)
Hypercholesterolemia is the main risk factor to threaten human health and geniposide has been found to have hypolipidemic functions. However, its underlying mechanism is not clear. In this study, we firstly confirmed the hypolipidemic functions of geniposide in C57BL/6 and
Ye-Jee Lee et al.
Journal of drug targeting, 29(1), 88-98 (2020-08-05)
Islet transplantation (ITx) is being developed as a treatment for type 1 diabetes mellitus, but hypoxic damage to transplanted islet grafts is an important factor affecting successful transplantation. To investigate the role of sirtuin-1 (SIRT1) under hypoxic injury in INS-1
Bi Chen et al.
Journal of thoracic disease, 8(11), 3063-3074 (2017-01-10)
Epithelial-mesenchymal transition (EMT) and cyclooxygenase-2 (COX-2) contribute to airway remodelling and inflammation in chronic obstructive pulmonary disease (COPD). Recent data suggest that the farnesoid X receptor (FXR), a nuclear receptor traditionally considered as bile acid-activated receptor, is also expressed in
Kristoffer Niss et al.
Molecular and cellular endocrinology, 517, 110923-110923 (2020-07-24)
Activated transcription factor (TF) farnesoid X receptor (FXR) represses glucagon-like peptide-1 (GLP-1) secretion in enteroendocrine L cells. This, in turn, reduces insulin secretion, which is triggered when β cells bind GLP-1. Preventing FXR activation could boost GLP-1 production and insulin
Qing Wu et al.
The Journal of clinical investigation, 131(9) (2021-05-04)
Intestinal farnesoid X receptor (FXR) signaling is involved in the development of obesity, fatty liver disease, and type 2 diabetes. However, the role of intestinal FXR in atherosclerosis and its potential as a target for clinical treatment have not been
Li-Min Liang et al.
Acta pharmacologica Sinica, 41(11), 1465-1475 (2020-04-29)
Peptide transporter 1 (PepT1), highly expressed on the apical membrane of enterocytes, is involved in energy balance and mediates intestinal absorption of peptidomimetic drugs. In this study, we investigated whether and how diabetes affected the function and expression of intestinal
Pengfei Qiao et al.
Oncology reports, 40(4), 2067-2078 (2018-08-15)
Colorectal cancer (CRC) is among the most common malignancies of the digestive system. Dysregulation of miRNAs and the farnesoid X receptor (FXR) are involved in the progression of CRC. In the present study, the effects of FXR and miR‑135A1 in
Amar Bahadur Singh et al.
Biochimica et biophysica acta. Molecular and cell biology of lipids, 1864(3), 358-371 (2018-12-24)
Long-chain acyl-CoA synthetase 1 (ACSL1) plays a pivotal role in fatty acid β‑oxidation in heart, adipose tissue and skeletal muscle. However, key functions of ACSL1 in the liver remain largely unknown. We investigated acute effects of hepatic ACSL1 deficiency on
Tomofumi Fujino et al.
The Journal of toxicological sciences, 45(1), 25-35 (2020-01-15)
In this study, we found that nuclear receptors FXR and LXR (originally characterized as regulatory factors involved in cholesterol/bile acid homeostasis) regulate the expression of Oct3/4, a marker for cell differentiation, in both normal renal-derived cell line HK-2 and renal
Xiao-Min Xin et al.
World journal of gastroenterology, 20(42), 15727-15735 (2014-11-18)
To investigate the effect of GW4064 on the expression of adipokines and their receptors during differentiation of 3T3-L1 preadipocytes and in HepG2 cells. The mRNA expression of farnesoid X receptor (FXR), peroxisome proliferator-activated receptor-gamma 2 (PPAR-γ2), adiponectin, leptin, resistin, adiponectin
Thomas A Kerr et al.
Hepatology research : the official journal of the Japan Society of Hepatology, 44(10), E218-E228 (2013-09-17)
Bile acid synthesis is regulated by nuclear receptors including farnesoid X receptor (FXR) and small heterodimer partner (SHP), and by fibroblast growth factor 15/19 (FGF15/19). We hypothesized that hepatic cysteine sulfinic acid decarboxylase (CSAD) (a key enzyme in taurine synthesis)
Teruo Miyazaki et al.
Journal of clinical biochemistry and nutrition, 64(2), 112-123 (2019-04-03)
Nuclear receptor farnesoid X receptor activation inhibits fatty acid synthesis through the liver X receptor-α-sterol regulatory element binding protein-1c pathway universally in animals, but also has human-specific crosstalk with the peroxisome proliferator-activated receptor-α. The effects of farnesoid X receptor-ligands on
Sarah Farr et al.
American journal of physiology. Gastrointestinal and liver physiology, 318(4), G682-G693 (2020-02-01)
Postprandial dyslipidemia is a common feature of insulin-resistant states and contributes to increased cardiovascular disease risk. Recently, bile acids have been recognized beyond their emulsification properties as important signaling molecules that promote energy expenditure, improve insulin sensitivity, and lower fasting
Jianlong Du et al.
The Journal of nutrition, 150(9), 2469-2477 (2020-07-03)
High linoleic acid (LA) intake leads to inflammation that adversely influences health in fish. However, whether the farnesoid X receptor (FXR) could be an effective target for regulating LA-induced inflammation remains unknown. The purpose of this study was to investigate
R Malivindi et al.
Reproduction (Cambridge, England), 156(3), 249-259 (2018-06-21)
The farnesoid X receptor alpha (FXR) is a bile acid sensor activated by binding to endogenous bile acids including chenodeoxycholic acid (CDCA). Although, FXR is expressed in male reproductive tissue, the relevance of the receptor on reproduction is scarcely known.
GW4064 attenuates lipopolysaccharide-induced hepatic inflammation and apoptosis through inhibition of the Toll-like receptor 4-mediated p38 mitogen-activated protein kinase signaling pathway in mice
Liu HM, et al.
International Journal of Molecular Medicine, 41(3), 1455-1462 (2018)
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