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Starting from the hypothesis that the linker portion
2022-06-02
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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br Cellular directionality To obtain a comprehensive underst
2022-06-02
Cellular directionality To obtain a comprehensive understanding of cell migration, it is essential to understand how cues from the cell’s external environment are relayed to the Simeprevir receptor cytoskeleton, so the cell can migrate towards the cue; a process herein referred to as cellular dir
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Selected GSNOR inhibitors were assessed for
2022-06-02
Selected GSNOR inhibitors were assessed for potential off-target activity with a panel of 54 transmembrane and soluble receptors, ion channels, and monoamine transporters. Off-target effects were estimated from the percent inhibition of receptor radio-ligand binding in the presence of 10μM of test c
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Neuromedin B To further investigate the relationship between
2022-06-02
To further investigate the relationship between the pro-neurogenic and therapeutic actions, we analyzed the effect of VP2.51 in the presence of the antimitotic agent TMZ. No overt side effects were found at the time of testing as assessed by direct observation of the behavior of the animals in their
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Recently a receptor for nicotinic
2022-06-02
Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f
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Another possible effect of niacin is
2022-06-02
Another possible effect of niacin is in altering immune cell trafficking; as it has been suggested that niacin therapy quells endothelial cell activation (Digby et al., 2010, Ganji et al., 2009) and thereby suppresses inflammatory cell recruitment (Wu et al. 2010). However, the impact of niacin on l
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Similar to GPR A activation of G protein coupled receptor
2022-06-02
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic KB SRC 4 synthesis receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al.,
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The mechanisms of action of MMF and DMF
2022-06-02
The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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Some clinical reports have suggested that galanin has
2022-06-01
Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]
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br Summary The presented results of the analysis
2022-06-01
Summary The presented results of the analysis of the unfolding of G-quadruplex and i-motif, which may appear within the telomeric DNA region, led to several important conclusions. Namely, determination of the work necessary to unfold of these structures, in biased molecular dynamics involving ste
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In the present studies we found
2022-06-01
In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 Etoricoxib australia and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) pro
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In recent years many studies
2022-06-01
In recent years, many studies have demonstrated that the release of endogenous FPR ligands can influence severe diseases associated with inflammation, including systemic inflammatory response syndrome (SIRS)20, 21 and cancers, such as glioblastoma as well as gastric and colorectal cancer 22, 23, 24.
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br Introduction GPR also known as
2022-06-01
Introduction GPR40 (also known as free fatty akt inhibitor receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and long-cha
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br Conflict of interest br Acknowledgments The research
2022-06-01
Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be
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methysergide The Rho family of GTPases is
2022-06-01
The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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