Concept

Cholestasis

Related publications (88)

TGR5-mediated bile acid sensing controls glucose homeostasis

Johan Auwerx, Kristina Schoonjans, Chikage Mataki, Hiroyasu Yamamoto, Lilia Noriega Lopez

TGR5 is a G protein-coupled receptor expressed in brown adipose tissue and muscle, where its activation by bile acids triggers an increase in energy expenditure and attenuates diet-induced obesity. Using a combination of pharmacological and genetic gain- a ...

2009

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

Johan Auwerx, Kristina Schoonjans

We describe here the biological screening of a collection of natural occurring triterpenoids against the G protein-coupled receptor TGR5, known to be activated by bile acids and which mediates some important cell functions. This work revealed that betulini ...

2009

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

Johan Auwerx, Kristina Schoonjans

In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords s ...

2009

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC

Ruben Hartkoorn

center dot Antiretroviral protease inhibitors such as lopinavir and saquinavir have been shown to be substrates of ABCB1. Co-administration with the potent ABCB1 and CYP3A4 inhibitor, ritonavir, has shown improved pharmacokinetics and subsequent therapeuti ...

2009

Targeting bile-acid signalling for metabolic diseases

Johan Auwerx, Kristina Schoonjans

Bile acids are increasingly being appreciated as complex metabolic integrators and signalling factors and not just as lipid solubilizers and simple regulators of bile-acid homeostasis. It is therefore not surprising that a number of bile-acid-activated sig ...

2008

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

Johan Auwerx, Kristina Schoonjans

Bile acids regulate nongenomic actions through the activation of TGR5, a membrane receptor that is G protein-coupled to the induction of adenylate cyclase. In this work, a training set of 43 bile acid derivatives is used to develop a molecular interaction ...

2008

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

Johan Auwerx, Kristina Schoonjans

TGR5, a metabotropic receptor that is G-protein-coupled to the induction of adenylate cyclase, has been recognized as the molecular link connecting bile acids to the control of energy and glucose homeostasis. With the aim of disclosing novel selective modu ...

2008

Liver-specific inactivation of Notch2, but not Notch1, compromises intrahepatic bile duct development in mice

Freddy Radtke

The Notch pathway is an evolutionary conserved, intercellular signaling pathway that plays an important role in cell fate specification and the embryonic development of many organs, including the liver. In humans, mutations in the Notch receptor ligand Jag ...

2008

c-Myc and its target FoxM1 are critical downstream effectors of constitutive androstane receptor (CAR) mediated direct liver hyperplasia

Sandra Eloise Kjeldsen, Christelle Dubey, Armin Ehninger

In the adult liver, 1,4-bis[2-(3,5-dichloropyridyloxy)] benzene (TCPOBOP), an agonist of the constitutive androstane receptor (CAR, NR1I3), produces rapid hepatomegaly in the absence of injury. In this study, we identify c-Myc as a gene induced by CAR and ...

2008

Methods for increasing cellular energy expenditure

Johan Auwerx

The present invention is directed to methods of treating a human for a variety of conditions by administering an agonist of the G protein coupled receptor TGR5. In addition, the invention includes methods for determining whether a test compound is likely t ...

2008

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