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The mechanism study demonstrated that
2022-07-20
The mechanism study demonstrated that BDNF is one of the fundamental mechanisms underlying JMJD2A effects during neuropathic pain. BDNF is a neurotrophin with essential functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels un
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There were hub genes identified by
2022-07-20
There were 11 hub genes identified by WGCNA among which KIBRA was the hub gene of the black module. The bioinformatics method is an effective and powerful tool to analyze mRNA ISRIB profiles and the related pathways. For instance, the lung cancer risk modules that were closely related to lung cance
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We have previously reported on the effects
2022-07-19
We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t
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Two different genes encode GSK isoforms
2022-07-19
Two different genes encode GSK-3 isoforms α and β that have very similar catalytic domains but significantly differ in their N- and C-termini. The α and β isoforms split from a common precursor approximately at the emergence of vertebrates, suggesting that at least one of the isoforms took on a new
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In addition during the preparation of this
2022-07-19
In addition, during the preparation of this manuscript, Oka et al. [7] demonstrated that LPA acts as receptor ligand for GPR35 and that LPA is more potent than KYNA in eliciting a calcium mobilization (EC50: 30nM vs. 39μM for LPA and KYNA, respectively). Other endogenous GPR35 ligands, therefore, mi
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The first described synthetic FFA active agonist GW phenoxyp
2022-07-19
The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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To further explain the energy differences
2022-07-19
. To further explain the energy differences between Group-A and Group-B, the average distances between ligands and the zinc cation were obtained from the last 1ns trajectory. It turns out that the members of group A were within the coordination distance of the zinc ion, whereas those of group B stay
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br Acknowledgments This work was
2022-07-19
Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE010200
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In conclusion we demonstrated that
2022-07-19
In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 pramipexole dihydrochloride results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This netwo
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The third generation cephalosporin antibiotics can cross the
2022-07-19
The third-generation cephalosporin ubiquitin conjugating enzyme can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when
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Increasing evidence has shown that blockade of glutamate upt
2022-07-19
Increasing evidence has shown that blockade of glutamate uptake leads to aberrant behavioral consequences. For example, intracerebroventricular (i.c.v) injection or microinjection of the GLT-1 inhibitor, dihydrokainic Amiloride HCl dihydrate synthesis (DHK), into the prefrontal cortex induces anhedo
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angiotensin ii receptor blockers Transmembrane AMPA receptor
2022-07-19
Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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As we showed earlier a to min incubation
2022-07-19
As we showed earlier [19], a 20- to 30-min incubation with 2mM t-BHP resulted in erythrocyte swelling, which was less in a Ca2+-containing medium. Given that this effect was abolished in the presence of the Gardos channel inhibitor CLT, as well as in media high in K+, we suggested the contribution f
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Although domain organization had been
2022-07-19
Although domain organization had been clearly delineated by the 4.3-Å structure of T4-γ-secretase [], atomic modeling of the side chains had to wait for the 3.4-Å structure []. In total, 598 residues in the transmembrane region and 632 residues in the ECD were modeled for the four components of huma
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Encouraged by the observation obtained from region
2022-07-19
Encouraged by the observation obtained from region A, we selected the structure of 1 as the next template to successively pursue the SAR on regions B-D of 1 (lower side of Fig. 2). Next, we turned attention to the external aromatic ring of 1 to verify the impact on the antagonistic activity and prep
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