(Q38541491)

4 September 2017

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title

Steroidal scaffolds as FXR and GPBAR1 ligands: from chemistry to therapeutical application (English)

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4 September 2017

3

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Angela Zampella

series ordinal

5

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Valentina Sepe

series ordinal

1

object named as

Valentina Sepe

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4 September 2017

Eleonora Distrutti

2

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4 September 2017

Stefano Fiorucci

series ordinal

4

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4 September 2017

publication date

1 July 2015

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Future Medicinal Chemistry

4 September 2017

published in

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4 September 2017

volume

7

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4 September 2017

issue

9

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4 September 2017

page(s)

1109-1135

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Identification of a nuclear receptor for bile acids

4 September 2017

cites work

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Bile acids: natural ligands for an orphan nuclear receptor

21 January 2018

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Endogenous bile acids are ligands for the nuclear receptor FXR/BAR

21 January 2018

1 reference

An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids.

21 January 2018

1 reference

Vitamin D receptor as an intestinal bile acid sensor

21 January 2018

1 reference

Identification of membrane-type receptor for bile acids (M-BAR)

21 January 2018

1 reference

Bile acid-induced arrhythmia is mediated by muscarinic M2 receptors in neonatal rat cardiomyocytes

21 January 2018

1 reference

Development of FXR, PXR and CAR agonists and antagonists for treatment of liver disorders

21 January 2018

1 reference

Bile acid-activated receptors in the treatment of dyslipidemia and related disorders

21 January 2018

1 reference

Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders

21 January 2018

1 reference

Targeting farnesoid X receptor for liver and metabolic disorders.

21 January 2018

1 reference

Role of nuclear receptors in lipid dysfunction and obesity-related diseases.

21 January 2018

1 reference

Farnesoid X receptor: from medicinal chemistry to clinical applications

21 January 2018

1 reference

Microbiota modification with probiotics induces hepatic bile acid synthesis via downregulation of the Fxr-Fgf15 axis in mice.

21 January 2018

1 reference

Dissociation of intestinal and hepatic activities of FXR and LXRα supports metabolic effects of terminal ileum interposition in rodents.

21 January 2018

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Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance

21 January 2018

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Intestinal farnesoid X receptor signaling promotes nonalcoholic fatty liver disease.

21 January 2018

1 reference

The bile acid receptor FXR is a modulator of intestinal innate immunity

21 January 2018

1 reference

Redundant pathways for negative feedback regulation of bile acid production

21 January 2018

1 reference

Coordinate transcriptional regulation of transport and metabolism

21 January 2018

1 reference

Enterohepatic bile salt transporters in normal physiology and liver disease

21 January 2018

1 reference

Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis

21 January 2018

1 reference

Tissue-specific actions of the metabolic hormones FGF15/19 and FGF21.

21 January 2018

1 reference

Primary biliary cirrhosis in adults

21 January 2018

1 reference

Cholestatic liver disease overlap syndromes

21 January 2018

1 reference

Primary sclerosing cholangitis

21 January 2018

1 reference

Liver diseases in pregnancy: diseases unique to pregnancy

21 January 2018

1 reference

Familial cholestasis: progressive familial intrahepatic cholestasis, benign recurrent intrahepatic cholestasis and intrahepatic cholestasis of pregnancy.

21 January 2018

1 reference

GPBA: a GPCR for bile acids and an emerging therapeutic target for disorders of digestion and sensation

21 January 2018

1 reference

Expression and function of the bile acid receptor GpBAR1 (TGR5) in the murine enteric nervous system.

21 January 2018

1 reference

The receptor TGR5 mediates the prokinetic actions of intestinal bile acids and is required for normal defecation in mice

21 January 2018

1 reference

Neuro-humoral signalling by bile acids and the TGR5 receptor in the gastrointestinal tract

21 January 2018

1 reference

Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1.

21 January 2018

1 reference

TGR5-mediated bile acid sensing controls glucose homeostasis

21 January 2018

1 reference

The bile acid receptor GPBAR-1 (TGR5) modulates integrity of intestinal barrier and immune response to experimental colitis

21 January 2018

1 reference

Mutational characterization of the bile acid receptor TGR5 in primary sclerosing cholangitis

21 January 2018

1 reference

The bile acid receptor TGR5 activates the TRPA1 channel to induce itch in mice.

21 January 2018

1 reference

Guggulsterone: an old approach to a new problem

21 January 2018

1 reference

A natural product that lowers cholesterol as an antagonist ligand for FXR.

21 January 2018

1 reference

Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump

21 January 2018

1 reference

Guggulipid for the treatment of hypercholesterolemia: a randomized controlled trial

21 January 2018

1 reference

The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand

21 January 2018

1 reference

Natural ligands for nuclear receptors: biology and potential therapeutic applications.

21 January 2018

1 reference

Structural basis for bile acid binding and activation of the nuclear receptor FXR

21 January 2018

1 reference

Pharmacophore-based discovery of FXR-agonists. Part II: identification of bioactive triterpenes from Ganoderma lucidum

21 January 2018

1 reference

Cycloartane triterpenoids from the stems of Schisandra glaucescens and their bioactivity.

21 January 2018

1 reference

Stigmasterol, a soy lipid-derived phytosterol, is an antagonist of the bile acid nuclear receptor FXR.

21 January 2018

1 reference

Marine sponge steroids as nuclear receptor ligands.

21 January 2018

1 reference

Sterols from a soft coral, Dendronephthya gigantea as farnesoid X-activated receptor antagonists

21 January 2018

1 reference

Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.

21 January 2018

1 reference

Discovery of sulfated sterols from marine invertebrates as a new class of marine natural antagonists of farnesoid-X-receptor

21 January 2018

1 reference

Theonellasterols and conicasterols from Theonella swinhoei. Novel marine natural ligands for human nuclear receptors.

21 January 2018

1 reference

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.

21 January 2018

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Quantitative NMR-derived interproton distances combined with quantum mechanical calculations of 13C chemical shifts in the stereochemical determination of conicasterol F, a nuclear receptor ligand from Theonella swinhoei

21 January 2018

1 reference

Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis

21 January 2018

1 reference

Preliminary structure-activity relationship on theonellasterol, a new chemotype of FXR antagonist, from the marine sponge Theonella swinhoei

21 January 2018

1 reference

Binding mechanism of the farnesoid X receptor marine antagonist suvanine reveals a strategy to forestall drug modulation on nuclear receptors. Design, synthesis, and biological evaluation of novel ligands.

21 January 2018

1 reference

6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.

21 January 2018

1 reference

Systematic review of herbs and dietary supplements for glycemic control in diabetes

21 January 2018

1 reference

Use of complementary and alternative medicine among persons with diabetes mellitus: results of a national survey.

21 January 2018

1 reference

Triterpenoids and rexinoids as multifunctional agents for the prevention and treatment of cancer.

21 January 2018

1 reference

Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic β cells

21 January 2018

1 reference

Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes

21 January 2018

1 reference

Anti-obesity and anti-hyperglycemic effects of the dietary citrus limonoid nomilin in mice fed a high-fat diet

21 January 2018

1 reference

Limonoids: overview of significant bioactive triterpenes distributed in plants kingdom

21 January 2018

1 reference

Citrus limonoids: analysis, bioactivity, and biomedical prospects

21 January 2018

1 reference

Abatacept in the treatment of lupus

21 January 2018

1 reference

Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease

21 January 2018

1 reference

Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis

21 January 2018

1 reference

Farnesoid X receptor agonist for the treatment of liver and metabolic disorders: focus on 6-ethyl-CDCA.

21 January 2018

1 reference

Efficacy of obeticholic acid in patients with primary biliary cirrhosis and inadequate response to ursodeoxycholic acid.

21 January 2018

1 reference

Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial

21 January 2018

1 reference

Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist.

21 January 2018

1 reference

Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.

21 January 2018

1 reference

Antiatherosclerotic effect of farnesoid X receptor

21 January 2018

1 reference

Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators

21 January 2018

1 reference

Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors.

21 January 2018

1 reference

FXR activation reverses insulin resistance and lipid abnormalities and protects against liver steatosis in Zucker (fa/fa) obese rats

21 January 2018

1 reference

Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mouse cholangiopathy model by promoting biliary HCO⁻₃ output

21 January 2018

1 reference

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.

21 January 2018

1 reference

Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.

21 January 2018

1 reference

Probing the Binding Site of Bile Acids in TGR5.

21 January 2018

1 reference

Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.

21 January 2018

1 reference

Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.

21 January 2018

1 reference

TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading

21 January 2018

1 reference

The novel compounds that activate farnesoid X receptor: the diversity of their effects on gene expression.

21 January 2018

1 reference

Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies

21 January 2018

1 reference

5beta-Cholane activators of the farnesol X receptor

21 January 2018

1 reference

Spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice

21 January 2018

1 reference

Spontaneous development of liver tumors in the absence of the bile acid receptor farnesoid X receptor

21 January 2018

1 reference

Deletion of IFNγ enhances hepatocarcinogenesis in FXR knockout mice

21 January 2018

1 reference

Effects of chemical modification of ursodeoxycholic acid on TGR5 activation

21 January 2018

1 reference

5Alpha-bile alcohols function as farnesoid X receptor antagonists

21 January 2018

1 reference

Structure-activity relationship of bile alcohols as human farnesoid X receptor agonist

21 January 2018

1 reference

Bile alcohols function as the ligands of membrane-type bile acid-activated G protein-coupled receptor

21 January 2018

1 reference

The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain

21 January 2018

1 reference

Intrahepatic cholestasis of pregnancy levels of sulfated progesterone metabolites inhibit farnesoid X receptor resulting in a cholestatic phenotype

21 January 2018

1 reference

Dose escalation pharmacokinetics and lipid lowering activity of a novel farnesoid X receptor modulator: 16-Dehydropregnenolone

21 January 2018

1 reference

Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation

21 January 2018

1 reference

Synthesis and evaluation of (18)F-labeled bile acid compound: a potential PET imaging agent for FXR-related diseases

21 January 2018

1 reference

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)

21 January 2018

1 reference

21 January 2018

Identifiers

DOI

10.4155/FMC.15.54

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4 September 2017

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