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In our study the changes in
2021-10-06
In our study, the changes in the α4 and δ subunit expression were accompanied by a significant increase in γ2 subunit expression in almost all analysed hippocampal structures in the fully kindled animals. In contrast, an acute injection of PTZ at a convulsive dose (55mg/kg) evoked a potent decrease
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Over the last decade intense efforts have been devoted
2021-10-03
Over the last decade, intense efforts have been devoted toward identifying IN inhibitors as potential drugs against HIV. Raltegravir and elvitegravir are integrase strand transfer inhibitors (INSTIs) that have been approved for therapy and dolutegravir is another INSTI that is currently in advanced
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In this study there is
2021-10-03
In this study, there is a limitation in the study of sex differences. Only female rats were used in our study. This is because the rats cannot urinate autonomously after SCI. Manual BKT140 emptying was needed until reflex bladder emptying was established (Lu et al., 2008, Ma et al., 2015). Because o
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Studies have demonstrated the paradoxical
2021-10-03
Studies have demonstrated the paradoxical role of HO-1 in tumorigenesis. At initial stages of carcinogenesis, it protects DNA by lowering the ROS-mediated mutational rate, but later, HO-1 promotes cancer cell survival and proliferation. One PDAC therapeutic strategy is to increase ROS production and
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The present study chose the fdh
2021-10-02
The present study chose the fdh gene, the homolog of mammalian GSNOR, to generate UAS-fdh and fdh double-stranded RNA interference (ds-RNAi) transgenic Drosophila. These transgenic models were used to study the effect of GSNOR activity modulation on visual learning and memory and to explore the poss
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GPR A a G protein
2021-10-02
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic devd [[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 inhi
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To further investigate its role in stresses tolerance
2021-10-02
To further investigate its role in stresses tolerance, OsGly I was overexpressed in transgenic rice. qRT-PCR and zymologic determination showed that mk2206 level of OsGly I and the glyoxalase I activity were significantly increased to different extent in the transgenic overexpression lines (Fig. 1,
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br Computational details and modeling All calculations were
2021-10-02
Computational details and modeling All calculations were performed using the density functional B3LYP [34] method, implemented in Gaussian03 program [35]. The structures of reactants, transition states, intermediates, and products were optimized using the 6-31+G(d) basis set for the H, C, N, O an
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The lack of inhibition of
2021-10-02
The lack of inhibition of K+ efflux in normal red cells reported by Fathallah et al. [16] was attributed by the authors to a lower level (about half) of membrane PKCα activity. In our experiments, single channel recording probably overcame this difficulty because of its molecular detection level. O
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130 ml The lack of biological activity http www apexbt com
2021-10-01
The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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It is an exciting time for translational histamine research
2021-10-01
It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams
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Hexokinases HXKs are major regulatory enzymes
2021-10-01
Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s
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br Structural studies of GCAP Recoverin was
2021-10-01
Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding mglur antagonist to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. The
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br GPR is a class
2021-10-01
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine lrrk2 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell signa
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In summary through medicinal chemistry
2021-10-01
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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