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In addition to acting as
2021-10-07
In addition to acting as the gatekeeper for the metabolic and antioxidant roles of glucose, HKs have also been found to regulate mPTP opening directly. First described in the cancer field, the high-affinity HK isoforms HK1 and HK2 are strongly anti-apoptotic when bound to the outer mitochondrial mem
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The following are the supplementary
2021-10-07
The following are the supplementary data related to this article. Introduction Target therapies have achieved significant gains in the fight against cancer, however, they are still a long way from providing generally curative treatments for the majority of cancers. Targeted agents can be used wi
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br Introduction Marijuana remains the most widely used
2021-10-07
Introduction Marijuana remains the most widely used illegal drug (Murray et al., 2007), and its validated targets include plasma membrane cannabinoid receptors, many of which are found in the central nervous system. The diverse physiological effects produced by marijuana and cannabinoid ligands s
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In this study for the first time
2021-10-06
In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal
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Ethanol decreased the value of desensitization for
2021-10-06
Ethanol decreased the τ-value of desensitization for GluR-Di. Coexpression of stargazin or γ4 further increased the effect of ethanol on desensitization (Fig. 3A, B). The highest ethanol concentration tested (200mM) reduced the τ-value by 16.5±4.9% (n=5) in the control receptors and by 29.3±9.3% (n=
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It is well known that TNF
2021-10-03
It is well known that TNF-α plays a pivotal role in the pathogenesis of RA. TNF-α influences diverse pathologic processes including joint destruction as well as inflammatory responses [16]. While TNF-α significantly increases the levels of sFas and mFas expression from FLS, IL-1β and IL-17 have mini
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Andexanet alfa works as a decoy for the FXa
2021-10-03
Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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Taking all these results into
2021-10-03
Taking all these results into account, we propose a model for the evolution of HIV DNA forms in blood during the natural history of HIV infection (Fig. 4a). During PHI, the labile linear and episomal HIV DNA forms are particularly abundant and mostly constitute evidence of active replication in rece
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br Introduction br The histaminergic system in
2021-10-03
Introduction The histaminergic system in the central nervous system The ruthenium red australia is continually processing information through aminergic systems present in the mammalian CNS such as the serotonergic, dopaminergic, noradrenergic and histaminergic systems which function by projec
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Multi targeting agents are of major interest
2021-10-03
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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The concentration of rapamycin that gave half
2021-10-03
The concentration of rapamycin that gave half-maximal induction of the expression of HO-1 and Prx-1 mRNA in normal hepatocytes was 0.05 μM, with maximal induction at about 0.1 μM rapamycin. While, at rapamycin concentrations higher than 0.1 μM, the degree of enzyme induction decreased, elevated expr
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br Role of dynamin in NPRA
2021-10-03
Role of dynamin in NPRA endocytosis In recent studies using 125I-ANP binding assay and confocal microscopy, we have examined the role of dynamin in the internalization and trafficking of NPRA in a stably transfected HEK-293 netarsudil australia [69]. Our findings indicated that ANP treatment of
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Barthi et al previously showed that curcumin inhibits IKK co
2021-10-02
Barthi et al.[43] previously showed that curcumin inhibits IKK complex activity and thus IκBα phosphorylation as well as the p65 nuclear translocation. Those data are in agreement with our results obtained by gel shift assays using GSTP1-1 promoter and consensus NF-κB probes. Moreover, luciferase ac
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Finally a potentially effective therapeutic approach is to
2021-10-02
Finally, a potentially effective therapeutic approach is to target the LDH enzymes that mediate bidirectional conversion of pyruvate into lactate. In particular, because LDHA is the predominant isoform expressed in glycolytic tumours, an array of LDHA-targeting compounds have been proposed and valid
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The GLU Epac transgenic mouse
2021-10-02
The GLU-Epac transgenic mouse enabled us to monitor cAMP responses to GPR119 ligands in individual primary cultured L-cells. Not all L-cells were found to be responsive to AR231453, suggesting there may be a subpopulation of L-cells that do not express functional GPR119. There was a tendency for sma
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