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One of the most common
2022-06-28
One of the most common dietary approaches against obesity-associated diseases is the increase in the consumption of ω3 polyunsaturated fatty acids [18], [19]. Since seminal paper by Bang and Dyeberg in which the low prevalence of coronary heart disease among the Inuit was associated with the high ma
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Next to their indirect effect on
2022-06-28
Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more
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To get a broader view of the
2022-06-28
To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat GLPG0634 receptor and confirm the inhibition of this in
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Different from stable transfection transient
2022-06-27
Different from stable transfection, transient expression was also found to yield γ-secretase with robust proteolytic activity []. Co-transfection of all four, but not any three, components of human γ-secretase yielded high expression levels. This observation strongly suggests the co-folding nature o
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The overall decrease in consummatory drive seen
2022-06-27
The overall decrease in consummatory drive seen in rodents treated with naltrexone in previous studies is in accordance with the effects seen with mice treated with SNAP 37889 in this study. While it may seem inappropriate to use a broad-acting drug like SNAP 37889 that suppresses overall consummato
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The results obtained here in int Gr and
2022-06-27
The results obtained here in int-Gr+/+ and int-Gr−/− mice suggested that Gr is required to maintain basal level of Fgf15 expression in the ileum, whereas DEX treatment is able to reduce Fgf15 mRNA in a Gr-independent manner. In previous in vitro studies we have already shown that GC are able to affe
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In addition several other considerations were made for
2022-06-27
In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty jak inhibitors receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were
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Herein we describe the design and optimization of
2022-06-27
Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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To further investigate if GPR was the
2022-06-27
To further investigate if GPR40 was the functional target of these phenylpropiolic Forskolin mg analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GP
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The Hippo pathway has been well established as a
2022-06-27
The Hippo pathway has been well established as a tumor suppressor pathway and is involved in many diverse biologic processes including cell growth, cell death, and organ size control in organisms, ranging from Drosophila to mammals [4]. Central to this pathway is a kinase cascade in which the Ste20-
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To validate the effects of the G a HMT inhibitors
2022-06-27
To validate the effects of the G9a HMT inhibitors on HMEC-1 dgat inhibitor and transcriptional responses we generated knockdown cells for G9a using an shRNA approach. Upon transduction of HMEC-1 and doxycycline activation of the shRNA, both G9a HMT mRNA and protein expression were effectively decre
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While reduced protein synthesis provides a
2022-06-27
While reduced protein synthesis provides a model to explain the long-term memory defects of kdm5 and kdm5 flies, new translation is not required for short-term memories. The chronic reduction in translation observed in mutant fly strains may, however, lower the levels of proteins necessary for short
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All these recent results show the interconnection
2022-06-27
All these recent results show the interconnection between the Hippo pathway as a tumor-suppressor on the one hand and its function as regulator of metabolic homeostasis on the other. Disruption of the Hippo pathway leads to cancer growth, which is often associated with pathological disturbances in t
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Aspartame l aspartyl l phenylalanine methylester is a dipept
2022-06-27
Aspartame (l-aspartyl l-phenylalanine methylester) is a dipeptide artificial sweetener that is widely used as a non-nutritive sweetener in various food products [1]. The increased market of dietary products and the development of new synthetic sweetening compounds have not been sufficiently explored
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An interesting question is why RhoF has such the slow
2022-06-27
An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino pitavastatin mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF, rather
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