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G protein coupled receptor GPCR ligands can be classified as
2022-02-09

G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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Entry into CNS is tightly regulated by highly
2022-02-08

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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Several studies have found decreased astroglial
2022-02-08

Several studies have found decreased astroglial and neuronal cell numbers and dexamethasone acetate 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
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In agreement with the results obtained from GluR A
2022-02-08

In agreement with the results obtained from GluR-A−/− mice, mice in which the NR1 subunit of the NMDA receptor has been selectively deleted from the CA3 subfield of the hippocampus displayed normal acquisition of the standard reference memory version of the watermaze task (Nakazawa et al., 2002), bu
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Because of its role in the cleavage
2022-02-08

Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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Determination of enzyme activity differs
2022-02-08

Determination of enzyme activity differs from other analytical procedures. In this 4-Aminobutyric acid synthesis case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed
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Tail group SAR of the imidazole
2022-02-08

Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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Alarelin Acetate To enhance the impact of GD as an immune ta
2022-02-08

To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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In C elegans KDM A appears to be involved in
2022-02-08

In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene
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In summary we have provided evidence that TA
2022-02-08

In summary, we have provided evidence that TA, a novel HATi, inhibits the acetylation of histone and non-histone proteins and activation of the mRNA expression of lipogenesis-related genes both in vitro and in vivo (Figure 8), indicating that inhibition of HAT activity by TA is necessary for the pre
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Metabolic adaptation is an important
2022-02-08

Metabolic adaptation is an important survival strategy for cancer cells within the hypoxic tumor environment. Under the condition of O2 limitation, metabolic pathways shift from energy-efficient oxidative phosphorylation to the anaerobic glycolysis pathway for the purpose of ATP generation [13,43].
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Multiple subsets of Breg cells in mice have been identified
2022-02-08

Multiple subsets of Breg cells in mice have been identified that could suppress the T cell-mediated response. However, a lack of consensus surface markers for Breg cells made it difficult to judge whether Breg cells are a special B cell subset or whether all β(1,3)-d-glucan synthase have an immuno-
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Here we examine the impact of
2022-02-08

Here we examine the impact of hypoxia on lake whitefish (Coregonus clupeaformis) during embryonic and larval development. Lake whitefish are a cold-water salmonid endemic to North America and are found from western Alaska, USA to eastern Labrador in Canada. Spawning occurs from late autumn to early
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To promote biomimetic growth of HAp Li
2022-02-08

To promote biomimetic growth of HAp, Li et al. [20] developed a technique to modify cellulose nanofibers using P2O5. It was ascertained that the negative phosphate groups bonded with Ca2+ through coordination bonds and subsequently guided the growth of the Ca–P crystals throughout the scaffolds. Sim
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Despite these studies little is known about the regulation o
2022-02-08

Despite these studies, little is known about the regulation of defence genes during AM root colonization. In the present study, we characterized the Ptc52 gene from tomato (named here as SlPtc52), a member of the gene family of non-heme oxygenases, and analysed its molecular characteristics. This ge
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