1,721,033 research outputs found
Probiotics VSL#3 protect against development of visceral pain in murine model of irritable bowel syndrome.
No full textThe plant sterol guggulsterone attenuates inflammation and immune dysfunction in murine models of inflammatory bowel disease.
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Targetting farnesoid-X-receptor: from medicinal chemistry to disease treatment.
No full textAbstract
The farnesoid X receptor (FXRalpha) is a metabolic nuclear receptor and bile acid sensor expressed in the liver and intestine. Physiological studies have shown that FXRalpha exerts regulatory roles in bile acids, lipid and glucose homeostasis. FXR ligands of steroidal and non-steroidal structure have been described. Both ligand groups have shown limitations in preclinical studies regarding their absorption, metabolism, target interactions and intrinsic toxicity. Inhibition of bile acid synthesis and basolateral transporters in the liver as well as reduction of high density lipoprotein (HDL) in the plasma are the major unwanted effect seen with these ligands. Several FXRalpha modulators are currently being generated with the aim of targeting FXRalpha isoforms by exploiting the relative unselectivity of the ligand binding domain of the receptor. Structure-activity relationship studies have shown that FXRalpha could be activated by structurally different ligands and that receptor occupancy by these ligands generate different patterns of gene activation as a results of specific conformational changes of the receptor or differential dislodgement of co-repressor or recruitment of co-activators. Generation of modulators that selectively target specific FXRalpha responsive elements are an interesting strategy to overcome the limitations of currently available FXR ligands
Reciprocal regulation of the bile acid-activated receptor FXR and the interferon-gamma-STAT-1 pathway in macrophages.
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Bile-acid-activated farnesoid X receptor regulates hydrogen sulfide production and hepatic microcirculation.
No full textThe Bile Acids Receptor TGR5 is an Essential Modulator of Intestinal Membrane Permeability and Exerts Anti-Inflammatory Activities in Rodent Model of Colitis
No full textEssential Role of DNAX Adaptor Protein 12 (DAP12) and Spleen Tyrosine Kinase (Syk) in Inflammation-Driven Immune Dysfunction in Rodent Model of Colitis
No full textFXR Activation Reverses Insulin Resistance and Protects Against NASH Development
No full textConference: Digestive Disease Week/110th Annual Meeting of the American-Gastroenterological-Association Location: Chicago, IL Date: MAY 30-JUN 04, 2009
Sponsor(s): Amer Gastroenterol Assoc
Accession Number: WOS:000275277202108
Document Type:Meeting Abstract
Language: Englis
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