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To help resolve the question of simple binding versus transp
2021-09-07

To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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Accordingly it is tempting to speculate that the
2021-09-07

Accordingly, it is tempting to speculate that the maintenance of a stimulus representation in the A2 state for a short period of time after the presentation of a specific stimulus (i.e. self-generated priming) may rely upon GluR-A-dependent synaptic plasticity. If this were the case, GluR-A BV6 wou
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Human Glucocorticoid Receptor hGR was first cloned in
2021-09-07

Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin
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Statins are recognized by their nephroprotective
2021-09-06

Statins are recognized by their nephroprotective effect (Chmielewski et al., 2002). The hepato- and nephroprotective effects of silymarin are also well studied (Alqasoumi, 2014, Mohamed et al., 2018). Several studies documented increasing phorbol myristate acetate of FXR by statins (Byun et al., 20
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In fish little information about Gpr is available We
2021-09-06

In fish, little information about Gpr84 is available. We have revealed that lipopolysaccharide (LPS) induces significantly up-regulation of zebrafish , and zebrafish overexpression markedly increased the LPS-stimulated production of the cytokine []. Here we expanded on these studies to further inv
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One effective approach to fine tuning
2021-09-06

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic ampk activator scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as
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Nifedipine We identified three genes KEAP NAA and ABCC
2021-09-06

We identified three genes—KEAP1, NAA38, and ABCC1/MRP1—as negative regulators of glutathione abundance in human cells. Like KEAP1, NAA38 appears to regulate NRF2 stability, as NAA38 deletion increased NRF2 protein levels and the expression of NRF2 target genes. NAA38 is a component of the NatC N-ter
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Sodium Nitroprusside mg Sirolimus rapamycin and everolimus b
2021-09-06

Sirolimus (rapamycin) and everolimus, both of which are mTOR inhibitors, are released by commonly used first- and second-generation DES. Considering the relatively high rates of the target vessel failure with currently available DES [12,14,16,45,46], there is a need for a novel drug strategy that pr
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More specific quantitative assays for DiXaIs are
2021-09-06

More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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In terms of outcome measures
2021-09-06

In terms of outcome measures, statistically significant differences were only observed in need for invasive mechanical ventilation (23% vs 46%, p-value 0.005) and in-hospital mortality (13% vs 37%, p-value 0.002). Both these outcomes were still statistically significant following adjustment for conf
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Regulation of gene expression in mammalian
2021-09-06

Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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Despite the importance of intratumor phenotypic
2021-09-06

Despite the importance of intratumor phenotypic heterogeneity for tumor progression and therapy resistance (Marusyk et al., 2012, Marusyk and Polyak, 2010), our understanding of regulators of this process and our ability to modulate them are very limited. Recent advances in genomic sequencing and si
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Consistent with a similar study we found
2021-09-06

Consistent with a similar study, we found economic status to be very important to domestic funding of HIV. Upper-middle-income and high-income countries are more likely to have fiscal space for health and be less reliant on external sources. Moreover, richer countries often attract larger cofinancin
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Assays can perform differently by genotype and under quantif
2021-09-06

Assays can perform differently by glucose transporter and under-quantification of HCV GTs has been seen with HCV assays [8], [9], [10], [11]. Under-quantification of GT4 has been reported in some early studies of the VERIS Assay [7], [12] where a bias greater than −0.5 log10IU/mL was seen. In two m
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The imidazopyridines and related imidazopyrimidines and were
2021-09-06

The imidazopyridines and related imidazopyrimidines – and – were constructed from the key amine intermediates – ( X=CH and Ar=2-FPh, X=N and Ar=2-FPh, X=CH and Ar=5-pyrimidine, X=CH and Ar=2-methyl-5-pyrimidine, and X=CF and Ar=2-methyl-5-pyrimidine). These were synthesized a modified Horner–Em
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