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
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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 ...
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 ...
23-Alkyl-substituted and 6,23-alkyl-disubstituted derivatives of chenodeoxycholic acid are identified as potent and selective agonists of TGR5, a G-protein coupled receptor for bile acids (BAs). In particular, we show that methylation at the C-23(S) positi ...
We generated and characterized a firefly luciferase reporter mouse for the nuclear receptor farnesoid X receptor (FXR). This FXR reporter mouse has basal luciferase expression in the terminal ileum, an organ with well-characterized FXRalpha signaling. In v ...
This paper describes ModelLib, a web-based platform for collecting models from different domains (e.g. electrical, mechanical) and levels of abstractions. Use cases for this tool are presented, which show how it can support the design~process of complex AM ...
Systems-on-Chips (SoCs) integrate more and more heterogeneous components: analog/RF/digital circuits, sensors, actuators, software. For the design of these systems very different description formalisms, or Models of Computation (MoCs), and tools are used f ...
This paper describes the development and application of a new unique tool to support designers to optimise the sustainability of urban neighbourhoods (SUNtool). In this the paper introduces (i) the software architecture, (ii) the integrated solver and rela ...
We explored the effects of bile acids on triglyceride (TG) homeostasis using a combination of molecular, cellular, and animal models. Cholic acid (CA) prevents hepatic TG accumulation, VLDL secretion, and elevated serum TG in mouse models of hypertriglycer ...
This position paper discusses the issues in design and development of a transaction support for Ada 95. Transactions and other fault tolerance mechanisms are reviewed, and their applicability in a concurrent programming language is analyzed. Possible ways ...
Cholesterol and bile acid metabolism is tightly controlled by nuclear receptors. The liver X receptor, an oxysterol-activated nuclear receptor, limits cholesterol accumulation in the body both by stimulating reverse cholesterol transport and by inhibiting ...