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Homophymine A, an anti-HIV cyclodepsipeptide from the sponge Homophymia sp.
TLDR
A new anti-HIV cyclodepsipeptide was isolated from a New Caledonian collection of the marine sponge Homophymia sp. Expand
Homophymines B-E and A1-E1, a family of bioactive cyclodepsipeptides from the sponge Homophymia sp.
TLDR
Nine new cyclodepsipeptides, homophymines B-E (2-5) and A1-E1 (1a-5a), were isolated from the polar extracts of the sponge Homophymia sp, featuring new polyketide-derived end groups, determined by interpretation of NMR and MS data. 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
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
Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands.
TLDR
A novel library of semisynthetic bile acid derivatives obtained by modifications on the cholane scaffold are described that might hold utility in the treatment of FXR and GP-BAR1 mediated disorders. Expand
Conicasterol E, a small heterodimer partner sparing farnesoid X receptor modulator endowed with a pregnane X receptor agonistic activity, from the marine sponge Theonella swinhoei.
TLDR
It is demonstrated that conicasterol E is an FXR modulator endowed with PXR agonistic activity and that this steroid might hold utility in treatment of liver disorders. Expand
Perthamides C-F, potent human antipsoriatic cyclopeptides
Abstract Two new cyclopeptides, perthamides E and F were isolated from the polar extracts of the sponge Theonella swinhoei . The new structures, featuring an unprecedented β-amino acid unit (AHMOA),Expand
Perthamides C and D, two new potent anti-inflammatory cyclopeptides from a Solomon Lithistid sponge Theonella swinhoei
Two new metabolites, perthamides C and D, have been isolated from the marine sponge Theonella swinhoei. Their structures were determined by interpretation of NMR and ESIMS data. All compoundsExpand
Modification on ursodeoxycholic acid (UDCA) scaffold. discovery of bile acid derivatives as selective agonists of cell-surface G-protein coupled bile acid receptor 1 (GP-BAR1).
TLDR
In vivo and in vitro pharmacological evaluation demonstrated that administration of compound 16 selectively increases the expression of pro-glucagon 1, a GP-BAR1 target, in the small intestine, while it had no effect on FXR target genes in the liver. Expand
Farnesoid X receptor modulators 2014-present: a patent review
TLDR
Despite the significant number of patent applications claiming steroidal and non-steroidal FXR agonists, several questions on their therapeutic potential in cholestasis and NASH remain open leaving a space for the development of novel compounds. Expand
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