Patented TGR5 modulators: a review (2006 - present). (Q38049636)

27 August 2017

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

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27 August 2017

22

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27 August 2017

12

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27 August 2017

1399-1414

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

27 August 2017

1 reference

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

The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation

21 January 2018

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

TGR5: an emerging bile acid G-protein-coupled receptor target for the potential treatment of metabolic disorders

21 January 2018

1 reference

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

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

21 January 2018

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

A G protein-coupled receptor responsive to bile acids

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Targeting bile-acid signalling for metabolic diseases

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

TGR5-mediated bile acid sensing controls glucose homeostasis

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity

21 January 2018

1 reference

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

Vitamin D receptor as an intestinal bile acid sensor

21 January 2018

1 reference

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

Identification of a nuclear receptor for bile acids

21 January 2018

1 reference

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

Bile acids: natural ligands for an orphan nuclear receptor

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Synthesis, characterization, and receptor interaction profiles of enantiomeric bile acids

21 January 2018

1 reference

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

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

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

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

1 reference

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

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

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

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

21 January 2018

1 reference

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

Effects of chemical modification of ursodeoxycholic acid on TGR5 activation

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

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

Oleanolic acid is a selective farnesoid X receptor modulator

21 January 2018

1 reference

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

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

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

Kupffer cells in non-alcoholic fatty liver disease: the emerging view.

21 January 2018

1 reference

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

NF-κB, inflammation, and metabolic disease.

21 January 2018

1 reference

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

Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation

21 January 2018

1 reference

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

The Physiology of Glucagon-like Peptide 1

21 January 2018

1 reference

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

Incretin-based therapy of type 2 diabetes mellitus

21 January 2018

1 reference

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

Dipeptidyl peptidase IV (DPP IV) inhibitors: A newly emerging drug class for the treatment of type 2 diabetes.

21 January 2018

1 reference

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

Weight and type 2 diabetes after bariatric surgery: systematic review and meta-analysis

21 January 2018

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Surgical treatment of obesity--weighing the facts

21 January 2018

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Serum bile acids are higher in humans with prior gastric bypass: potential contribution to improved glucose and lipid metabolism

21 January 2018

1 reference

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

Serum bile acid along with plasma incretins and serum high-molecular weight adiponectin levels are increased after bariatric surgery.

21 January 2018

1 reference

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

Obesity, inflammation, and atherosclerosis

21 January 2018

1 reference

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

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

21 January 2018

1 reference

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

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

21 January 2018

1 reference

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

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

1 reference

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

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

21 January 2018

1 reference

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

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

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DOI

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27 August 2017

1 reference