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In this study we explore different mathematical
2022-01-12
In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed
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It has been shown that GPR receptors
2022-01-12
It has been shown that GPR55 receptors coupled to G12/13 proteins down-regulate reactive oxygen species (ROS) production and degranulation in human neutrophils [9]. MCs degranulation stimulated by IgE/Ag also requires the generation of ROS [64]; therefore, the possibility to explore the inhibitory a
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br Conflict of interest br Acknowledgment This work was
2022-01-12
Conflict of interest Acknowledgment This work was supported by National Program on Key Basic Research Project of China (No. 2013CB127305); The National Natural Science Foundation of China (No. 314020785); Hubei Provincial Creative Team Project of Agricultural Science and Technology (No. 2007-6
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A considerable body of evidence suggests that
2022-01-11
A considerable body of evidence suggests that alcohols, volatile anesthetics and inhaled drugs of abuse act at discrete sites on glycine and GABAA receptors, specifically within circumscribed protein pockets (Mascia et al., 2000, Mihic et al., 1997, Beckstead et al., 2000). An amino ulixertinib synt
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Structural analysis of the MD
2022-01-11
Structural analysis of the MD-open state unveils that the transmembrane domain features a symmetric organization of the pore-lining helices M2 similar to the semi-open structure but with a local asymmetry at the constriction point, which is critical for chloride permeation. The atomistic simulations
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br Preclinical development of GIP agonists
2022-01-11
Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a
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The general aim of our in vitro experiments was to
2022-01-11
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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Irinotecan HCl Trihydrate mg br Genetic manipulation variati
2022-01-11
Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors
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However at variance with the well studied R form of
2022-01-11
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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The current lack of effective treatments for
2022-01-11
The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th
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On the other hand G a GLP could also alter
2022-01-11
On the other hand, G9a/GLP could also alter neuronal function without directly altering the transcription level of particular plasticity-related protein: the consolidation of early-LTP to late-LTP, as well as the reversal of mGluR-LTD by G9a/GLP inhibition required PKMζ translation and its downstrea
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Several studies have indicated that PLD
2022-01-11
Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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The molecular mechanisms underlying spindle orientation are
2022-01-11
The molecular mechanisms underlying spindle orientation are still largely unknown. Budding yeast has been used to study spindle positioning and asymmetric cell division. Indeed, after cytokinesis, daughter cells have different sizes. The cell division plane is established early in the cell cycle and
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Despite the similarities there are some differences between
2022-01-11
Despite the similarities, there are some differences between the augmentation by hypoxia and that by thymoquinone. While in porcine coronary arteries they both depend on calcium sensitization mediated by ROCK12, 32, 33, L-type calcium channels are involved only in thymoquinone-induced augmentation.
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br Materials and methods br Results
2022-01-11
Materials and methods Results Discussion GSK-3 overexpression diminishes neurogenesis (Fuster-Matanzo et al., 2013, Kondratiuk et al., 2013, Sirerol-Piquer et al., 2011), while the inhibition of GSK-3 with lithium or valproate enhances neurogenesis, as measured by cell proliferation, the nu
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