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To shed more light on
2021-10-09

To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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Several studies have found decreased astroglial
2021-10-09

Several studies have found decreased astroglial and neuronal cell numbers and Pradaxa damage after OP exposure. Neuronal loss and brain lesions increase proportionally to the severity and duration of OP-induced seizures (Albuquerque et al., 2006, Carpentier et al., 2000, Gullapalli et al., 2010, My
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GSK3787 Considerable evidence links sustained GCG administra
2021-10-09

Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms
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It is considered that activations of MMP and
2021-10-08

It is considered that activations of MMP-2 and MMP-9 are closely related to progression process of cancer cells, such as invasion and metastasis [22], [23]. In fibrosarcoma cells, GPR40 suppressed not only MMP-2 and MMP-9 activations, but also cell motile and invasive activities, suggesting GPR40 ne
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In the present study we
2021-10-08

In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip
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Finally worth of mention are few
2021-10-08

Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Isoniazid library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series o
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br Materials and methods br Results and
2021-10-08

Materials and methods Results and discussion We recently found that the GlyT1 N-terminal and C-terminal sequences could be modified by phophorylation, or partially lost under pathological conditions by calcium-dependent proteolysis (Baliova and Jursky, 2005, Baliova and Jursky, 2010). While re
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Elimination of the Q R bridge significantly affected
2021-10-08

Elimination of the Q234–R244 bridge significantly affected the protein PDK1 inhibitor but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially retained the bound z
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br Materials and methods br Conflicts of
2021-10-08

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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Numerical models of blood regulation provide insight into th
2021-10-08

Numerical models of blood regulation provide insight into the interaction of the cellular-level and macro-scale phenomena studied in silico, a term referring to computer simulations of the dynamics of complex biological systems as opposed to in vivo or in vitro experimental studies. These in silico
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NMDARs are glutamate gated ionotropic receptors
2021-10-07

NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo
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GS-7340 fumarate Both anxiety like behavior and sucrose pre
2021-10-07

Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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br Anti Factor Xa methods for DiXaIs measurement in plasma
2021-10-07

Anti-Factor Xa methods for DiXaIs measurement in plasma Concerning Anti-Factor Xa methods, there is an excellent correlation between the 1-stage and 2-stage Anti-assays as shown in Fig. 6, and the concentrations measured are very similar with all methods. These methods and the DiXaI concentration
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The stud http www apexbt
2021-10-07

The study was supported by Science Foundation for the Youth Scholars of Hubei Provincial Department of Education for Science and technology research program (No.: Q2017007). Introduction Chlorpyrifos is an organophosphate (OP) insecticide widely used in a variety of food crops to control a great
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br Materials and methods br Results br Discussion GPR
2021-10-07

Materials and methods Results Discussion GPR35 expression has been identified within discrete regions of the nervous system, including the spinal cord [[43], [44], [45], [46], [47], [48]]. Importantly, GPR35 is expressed not only in neurons but also in spinal glial cells [43]. Unfortunately
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