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Probiotics Modulate Intestinal Expression of Nuclear Receptor and Provide Counter-Regulatory Signals to Inflammation-Driven Adipose Tissue Activation
TLDR
Mesenteric adipose tissue from rodent colitis and Crohn's disease is metabolically active and shows inflammation-driven regulation of PPARγ, FXR and leptin, and probiotics correct the inflammation- driven metabolic dysfunction. Expand
Farnesoid X receptor suppresses constitutive androstane receptor activity at the multidrug resistance protein-4 promoter.
TLDR
The view that FXR activation in obstructive cholestasis might worsen liver injury by hijacking a protective mechanism regulated by CAR is supported and a new molecular explanation to the pathophysiology of cholESTasis is provided. Expand
VSL#3 Resets Insulin Signaling and Protects against NASH and Atherosclerosis in a Model of Genetic Dyslipidemia and Intestinal Inflammation
TLDR
Low grade intestinal inflammation drives a transition from steatosis to steatohepatitis and worsens the severity of atherosclerosis in a genetic model of dyslipidemia. Expand
Efficacy of the CCR5 Antagonist Maraviroc in Reducing Early, Ritonavir-Induced Atherogenesis and Advanced Plaque Progression in Mice
TLDR
Exposure to maraviroc limits the evolution and associated systemic inflammation of ritonavir-induced atherosclerotic in ApoE−/− mice and inhibits plaques development in a late model of atherosclerosis in which dyslipidemia plays the main pathogenic role, and could benefit HIV-positive patients with residual chronic inflammation despite a suppressive antiretroviral therapy. Expand
Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors.
TLDR
It is shown that compound 19 activates GP-BAR1, FXR, and FXR regulated genes in the liver, increases the intracellular concentration of cAMP, and stimulates the release of the potent insulinotropic hormone GLP-1, resulting in a promising drug candidate for the treatment of metabolic disorders. Expand
Theonellasterols and conicasterols from Theonella swinhoei. Novel marine natural ligands for human nuclear receptors.
TLDR
Pharmacological and structure-activity relationship analysis demonstrate that these natural polyhydroxylated steroids are potent ligands of human nuclear pregnane receptor (PXR) and modulator of farnesoid-X-receptor (FXR). Expand
CCR5 Antagonism by Maraviroc Reduces the Potential for Gastric Cancer Cell Dissemination.
TLDR
It is shown that C CR5 is mechanistically involved in dissemination of gastric cancer cells, suggesting that small molecule inhibitors of CCR5 might be exploited for their anticancer potential. Expand
Polyhydroxylated sterols from the Indonesian soft coral Sinularia sp. and their effect on farnesoid X-activated receptor
TLDR
These results represent the first evaluation of soft coral steroids for interaction with nuclear receptors and qualify gorgosterol (7) as a new chemotype of FXR antagonist. Expand
The HIV Matrix Protein p17 Subverts Nuclear Receptors Expression and Induces a STAT1-Dependent Proinflammatory Phenotype in Monocytes
TLDR
P17 is identified as a novel target in HIV therapy and grounds the development of anti-p17 small molecules or vaccines because of the activation of this pathway leads to a simultaneous dysregulation of immune and metabolic functions. Expand
Discovery That Theonellasterol a Marine Sponge Sterol Is a Highly Selective FXR Antagonist That Protects against Liver Injury in Cholestasis
TLDR
FXR antagonism in vivo results in a positive modulation of MRP4 expression in the liver and is a feasible strategy to target obstructive cholestasis. Expand
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