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In order to elucidate the mechanisms behind the observed cha
2022-05-24

In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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The rat model was validated with another agonist
2022-05-24

The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L
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With this goal in mind we proceeded to explore the
2022-05-24

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in activ
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br Glycoengineering br The Omics perspective The publication
2022-05-23

Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO Phenyl sulfate australia for improved glycoprot
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Growing evidence suggests that the glycine site seems
2022-05-23

Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it EPZ031686 has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). Moreover, mice w
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luciferin definition ICH induced striatal lesion produced a
2022-05-23

ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino luciferin definition transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain
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Methods br Results br Discussion In this report
2022-05-23

Methods Results Discussion In this report, the therapeutic effect of a GCGR antagonistic antibody REMD2.59 was tested in 2 mechanistically divergent disease models of heart failure without confounding defects in global metabolism. Based on histological and functional analyses in both MI-injur
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Although in in vitro analyses GANT sensitized
2022-05-23

Although in in vitro analyses GANT61 sensitized Daoy estrogen receptors to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced within
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The biological actions of ghrelin are mainly
2022-05-23

The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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br Materials and methods br Conflicts of
2022-05-23

Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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Gap junctions mediate electrical coupling between
2022-05-23

Gap junctions mediate electrical coupling between cells by conducting direct ionic currents and thereby modulate their electrical activity (Hormuzdi et al., 2004). In the nervous system, electrical coupling organizes network activity by amplifying and synchronizing neuronal firing (Galarreta and Hes
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GSIs were shown to effectively decrease A levels
2022-05-23

GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel
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The knowledge that piroxicam competes with ligands
2022-05-23

The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re
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Ning et al showed that LPC
2022-05-23

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Introduction Terpenoids also known as isoprenoids constitute
2022-05-23

Introduction Terpenoids, also known as isoprenoids, constitute a large family of natural products comprising at least 22,000 compounds and play diverse and important roles in plants as hormones, phytosynthetic pigments, and electron carriers [1], [2]. In addition, volatilized terpenoids contribute
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