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We started our investigation by
2022-09-08
We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition.
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Results of studies on fish FBPase are somewhat confusing alt
2022-09-07
Results of studies on fish FBPase are somewhat confusing: although fishes skeletal muscles possess relatively high FBPase activity (Knox et al., 1980, Lushchak et al., 2001) and the isozyme present therein has kinetic properties typical to all vertebrates muscle FBPases (Rosenmann et al., 1977), inv
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br Materials and methods br Results The immunoblot analysis
2022-09-07
Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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The deduced amino acid sequences of all
2022-09-07
The deduced amino CD 2665 sequences of all scIPPSs display high similarity, and sequence alignments reveal seven conserved regions [2]. Regions II and VI contain the substrate-binding regions, with two characteristic aspartate-rich motifs (DDx(xx)xD; where x represents any amino acid residue). Regi
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br Materials and methods br Results br Discussion ERK
2022-09-07
Materials and methods Results Discussion ERK5 signaling and its regulation has gained focus in recent years specially in the subject of cardiovascular biology, where this kinase plays a key role in angiogenesis and maintenance of blood vessel integrity [18,20,34,35]. The signaling pathways
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br Conclusions Our in vitro and
2022-09-07
Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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br Statistical analysis The mean standard
2022-09-07
Statistical analysis The mean, standard deviation, median, range, frequency, and percentage were used for data description. The chi-square (x2) test was used for analyses the differences in categorical variables in the 2-way table. Overall survival (OS) was defined as the time interval between t
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We are pursuing a hit to lead medicinal chemistry
2022-09-06
We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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Recent evidence suggests that HCA can also mediate
2022-09-06
Recent evidence suggests that HCA2 can also mediate antineuroinflammatory effects [63]. Studies in this field were initiated when monomethyl fumarate, the metabolite of DMF, was shown to be an agonist of HCA2[5]. DMF at the same time was shown to not only have beneficial effects in the treatment of
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The activation of AKT and ERK
2022-09-06
The activation of AKT and ERK1/2 results in the stabilization and increase in the co-transcriptional function of β-catenin [31], [32], [33]. Here, (R,R′)-MNF was found to reduce the levels of phospho-active AKT and ERK, which, in turn, may regulate the abundance and signaling potential of β-catenin.
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The atherosclerosis development requires additional pro infl
2022-09-06
The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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Additionally OsGly I overexpressing transgenic rice plants h
2022-09-05
Additionally, OsGly I-overexpressing transgenic rice plants had higher grain yields than WT (Table 2). Although there were no significant differences in the number of effective panicles per plant, panicle length, grain numbers per panicle, or 1000-grain weight between WT and transgenic plants, the s
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Entry into CNS is tightly regulated by
2022-09-03
Entry into CNS is tightly regulated by highly dynamic barriers, namely, the BBB, the blood-CSF barrier, and the arachnoid epithelium (Abbott et al., 2010; Yasuda et al., 2013). Similar barriers also exist within the CNS including the ependymal barrier as well as the cellular membrane barriers of the
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We observed the reduced expression of the
2022-09-03
We observed the reduced expression of the GluN2a subunit in the temporal and entorhinal cortexes and ventral hippocampus, which may result in the predominance of GluN2b-containing NMDA receptors during the latent period. Previously, using the same model, we revealed the reduction of the GluN2a/GluN2
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br Vertebrate steroid receptor evolution br Conclusion The t
2022-09-03
Vertebrate steroid receptor evolution Conclusion The teleost WGD event resulted in the duplication of the vertebrate GR and MR and two GRs have been retained in the majority of teleost fish studied so far. The molecular basis for this retention has yet to be fully understood. The cloning of th
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