(Q38049636)

27 August 2017

title

Patented TGR5 modulators: a review (2006 - present). (English)

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27 August 2017

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Antimo Gioiello

1

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Antonio Macchiarulo

object named as

Antonio Macchiarulo

4

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author name string

Emiliano Rosatelli

2

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27 August 2017

Roberto Nuti

3

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27 August 2017

Roberto Pellicciari

5

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27 August 2017

language of work or name

English

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publication date

6 October 2012

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Expert Opinion on Therapeutic Patents

27 August 2017

published in

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27 August 2017

volume

22

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27 August 2017

issue

12

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27 August 2017

page(s)

1399-1414

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Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease

27 August 2017

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1 reference

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A G protein-coupled receptor responsive to bile acids

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The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders

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Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation

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

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Expression and function of the bile acid receptor TGR5 in Kupffer cells

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TGR5-mediated bile acid sensing controls glucose homeostasis

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Gender-dependent effect of Gpbar1 genetic deletion on the metabolic profiles of diet-induced obese mice

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Hydrophobic bile salts inhibit gallbladder smooth muscle function via stimulation of GPBAR1 receptors and activation of KATP channels.

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The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling

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The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor κ light-chain enhancer of activated B cells (NF-κB) in mice

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21 January 2018

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Molecular field analysis and 3D-quantitative structure-activity relationship study (MFA 3D-QSAR) unveil novel features of bile acid recognition at TGR5.

21 January 2018

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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

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

21 January 2018

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Effects of chemical modification of ursodeoxycholic acid on TGR5 activation

21 January 2018

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

21 January 2018

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TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading

21 January 2018

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

21 January 2018

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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

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Oleanolic acid is a selective farnesoid X receptor modulator

21 January 2018

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

21 January 2018

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Redefining the TGR5 triterpenoid binding pocket at the C-3 position

21 January 2018

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Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists

21 January 2018

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Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.

21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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The Physiology of Glucagon-like Peptide 1

21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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Bile acid-induced TGR5-dependent c-Jun-N terminal kinase activation leads to enhanced caspase 8 activation in hepatocytes

21 January 2018

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Involvement of membrane-type bile acid receptor M-BAR/TGR5 in bile acid-induced activation of epidermal growth factor receptor and mitogen-activated protein kinases in gastric carcinoma cells

21 January 2018

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

21 January 2018

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Hypertrophic cardiomyopathy and dysregulation of cardiac energetics in a mouse model of biliary fibrosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2012.733000

10.1517/13543776.2012.733000

21 January 2018

Identifiers

DOI

1 reference

27 August 2017

1 reference