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The overall decrease in consummatory drive seen in
2021-09-26

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
2021-09-26

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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br Introduction More than structurally different
2021-09-26

Introduction More than 30,000 structurally different isoprenoids, such as steroids, carotenoids, prenyl side-chain of quinones, prenyl proteins, and natural rubber, exist in nature. In a biosynthetic pathway, linear prenyl diphosphates are common structures as a precursor of isoprenoids, as shown
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br Conflict of interest br Acknowledgment M
2021-09-26

Conflict of interest Acknowledgment M.D.P. lab is supported by the EPFL and Swiss National Science Foundation (SNF grant No. 200020_157153). Introduction As amyloid-β peptide (Aβ) accumulation in the idasanutlin sale starts in the very early stages of Alzheimer’s disease (AD) pathology (B
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With LML methyl oxo dihydropyridazin yl piperidin yl
2021-09-26

With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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Whereas binding of activated RhoA to the PH domains of
2021-09-24

Whereas binding of activated RhoA to the PH domains of the RhoGEFs is proposed to mediate positive feedback regulation (Chen et al., 2010b, Medina et al., 2013), the sequestration of p190RhoGEF by activated Rac1 reveals a novel putative physiological role, that is to utilize Rac1 to directly drive r
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br Action of GPR in metabolically active tissues In addition
2021-09-24

Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.
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GPR A a G protein coupled receptor located mainly on
2021-09-24

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic libraries [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-mediated
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At the second step blind docking
2021-09-24

At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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Acknowledgments br Introduction Type diabetes mellitus T DM
2021-09-24

Acknowledgments Introduction Type 2 diabetes mellitus (T2DM) is caused by relative insulin deficiency or insulin resistance in peripheral tissues. The clinical management of T2DM is achieved by controlling blood glucose levels. Current therapies available for treatment of T2DM include biguanides
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Next we asked how a common
2021-09-24

Next, we asked how a common activation marker of fibroblasts, Acta2, defined gene expression signatures in alveolar airspaces by using Acta2-mKO1 reporter mice (Fig. 2A). In the lungs of Acta2-mKO1 mice, mKO1 was expressed in smooth muscle cells and mesenchymal cells in Protease Inhibitor Cocktail (
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pde-5 inhibitors br Methods br Results Top panels of the Fig
2021-09-24

Methods Results Top panels of the Fig. 1 show the conventional representation of the predicted values of TL,CO according to ERS’93 and GLI′17 as a function of age and keeping the height constant (160 cm, panel A and 190 cm, panel B). This figure shows that the GLI-‘17 predicted values of TL,CO
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For many plasma membrane receptors including GPCRs
2021-09-24

For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an
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The general aim of our in
2021-09-24

The general aim of our in vitro experiments was to analyze the patterns of ghrelin and GHSR-1a expression in the mammary glands of dairy goats during pregnancy and to examine the direct effect of ghrelin on cell proliferation in cultured MECs of pregnant dairy goats. For this purpose, we cultured go
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We next investigated whether pharmaceutical inhibition of th
2021-09-24

We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not signifi
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