Farnesoid X receptor agonist
Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra and extrahepatic cholestasis
... extrahepatic obstructive cholestasis. In this model, the drainage of bile from the liver to the duodenum is blocked, resulting in the accumulation of bile in the liver. In both models we saw compensatory changes in ...
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Characterization of EDP-305, a Highly Potent and Selective Farnesoid X Receptor Agonist, for the Treatment of Non-alcoholic Steatohepatitis
... FXR, Farnesoid X Receptor; H&E, Haemotoxylin and Eosin; HDL, high density lipoprotein; HEK, human embryonic kidney; HFD, high fat diet; HSC, hepatic stellate cell; Il-1β, interleukin 1β; LDL, low ...
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Farnesoid X receptor agonist INT-767 attenuates liver steatosis and inflammation in rat model of nonalcoholic steatohepatitis
... nuclear receptor superfamily that binds to and interferes with the positive regulation of gene expression by other nuclear receptors including liver receptor homolog-1 on the target gene such as ...
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Upregulation of microRNA-23b-3p induced by farnesoid X receptor regulates the proliferation and apoptosis of osteosarcoma cells
... Farnesoid X receptor (FXR, NR1H4), which serves as a ligand-activated transcription factor with multiple func- tions, is mainly expressed in the liver, intestine, kidneys, and adrenal glands [19, ...
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Inhibitory Effects of Bile Acids and Synthetic Farnesoid X Receptor Agonists on Rotavirus Replication
... Effects of various bile acids on rotavirus replication in cells. Among the bile acids tested, CDCA and DCA significantly reduced the replication of rotaviruses (Wa and SA11 strains) at 100 M compared to that seen with ...
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TO901317 regulating apolipoprotein M expression mediates via the farnesoid X receptor pathway in Caco-2 cells
... nuclear receptor activated by the FXRs that interacts physically with many nuclear receptors including ...LXR/FXR agonist that activates FXR more efficiently than its natural ligand, the bile acids ...
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Farnesoid X receptor agonists attenuate colonic epithelial secretory function and prevent experimental diarrhoea in vivo
... these transport proteins under basal conditions. However, we found that treatment with GW4064 reversed agonist-induced inhibition of NHE3 activity. This is important since many prose- cretory agonists, typi fi ed ...
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Effective fecal microbiota transplantation for recurrent Clostridioides difficile infection in humans is associated with increased signalling in bile acid farnesoid X receptor fibroblast growth factor pathway
... FXR agonist (CDCA) is offset by increased levels of two moderate FXR agonists (DCA and LCA), 21 with a net upregulation of the ileal FXR-FGF pathway following successful ...
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Intestinal farnesoid X receptor signaling promotes nonalcoholic fatty liver disease
... synthetic agonist GW4064 increased HFD-induced lipid accumulation in the liver, partially due to a significant reduction in BA pool size and energy expenditure ...FXR agonist (54), which likely reflects the ...
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Farnesoid X receptor is essential for normal glucose homeostasis
... In contrast to the results with CA feeding, we did not observe similar effects on gluconeogenic gene expression or glucose metabolism in several different treatments with the synthetic FXR agonist GW4064 over ...
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<p>Evaluating the Therapeutic Potential of Cenicriviroc in the Treatment of Nonalcoholic Steatohepatitis with Fibrosis: A Brief Report on Emerging Data</p>
... Although early clinical data support direct antifibrotic effects of CVC, effects on metabolic components of NAFLD and NASH have been limited. Combination approaches to incorporate novel investigational agents tar- geting ...
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Farnesoid X Receptor and Its Ligands Inhibit the Function of Platelets
... incubation with GW4064 (1,10 M) or vehicle (containing DMSO (0.1% (v/v)) for 5 min. Blood was perfused for 10 min, after which thrombus development was assessed by measurement of fluorescence intensity. In comparison ...
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PKCλ in liver mediates insulin induced SREBP 1c expression and determines both hepatic lipid content and overall insulin sensitivity
... were generated by homologous recombination (K. Aki- moto et al., unpublished observations). Mice that express Cre recombinase under the control of the albumin gene promoter (Alb-Cre mice) (13) were pro- vided by D. ...
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A retinoid X receptor partial agonist attenuates pulmonary emphysema and airway inflammation
... Liver X receptors; MMP-9: Matrix metalloproteinase-9; NF- κ B: Nuclear factor- κ B; NRs: Nuclear receptors; PBS: Phosphate buffered saline; PPARs: Peroxisome proliferator-activated receptors; PPE: Porcine pancreas ...
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Medicinally active dihalocyclopropanes
... Estrogen Receptor Modulators ...estrogen receptor in breast tissue, however, in other tissues such as the endometrium, it behaves as an ...mixed agonist and antagonist activities of Tamoxifen are ...
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The effect of receptor density on the binding and functional properties of the human adenosine A1 receptor
... a receptor with more than one-class of G-protein (for example see Pohjanoksa et ah, ...Ai receptor can co-immunoprecipitate with [^^SjOTPyS bound GoCs subunits and stimulate adenylyl cyclase in pertussis ...
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Differential regulation of renal phospholipase C isoforms by catecholamines
... phospholipase C (PLC) activity, but whereas dopamine produces a natriuresis, NE has an antinatriuretic effect. To determine if catecholamines differentially regulate the expression of PLC isoforms, we infused fenoldopam, ...
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Influence of Flaxseed on Some Biochemical Factors, Antioxidant Activity and Expression of ABCG5 and ABCG8 Genes in the Liver of Diabetic Rat
... Liver X receptors (LXRs) are a part of the nuclear receptor family which are controlled lipid carbohydrate ...liver X receptor agonist improved elimination of sterol, reduced ...
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Activation of the Farnesoid X-receptor in breast cancer cell lines results in cytotoxicity but not increased migration potential
... Cell viability was assessed by the 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide (MTT) assay, as previously described [22]. Briefly, breast cancer cell lines were plated in 96-well tissue culture flasks at ...
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Complement Receptor Targeted Liposomes Encapsulating the Liver X Receptor Agonist GW3965 Accumulate in and Stabilize Atherosclerotic Plaques
... liver X receptor (LXR) agonist GW3965 is a promising therapeutic compound, since it induces reverse cholesterol transport in foam ...p32 receptor expressed on foam ...
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