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One of the main clinical
2021-09-17

One of the main clinical issues of ABCB1, together with its impact on intestinal absorption, concerns its location at the BBB. Indeed, ABCB1 has been identified in the luminal side of endothelial cells and in the abluminal side of astrocyte endfeet processes of the CNS microvasculature [[36], [37],
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Having shown that some of
2021-09-17

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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We observed the reduced expression of the GluN a
2021-09-17

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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In prostate cancer PCa glucose
2021-09-17

In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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This GluR A independent mechanism by
2021-09-17

This GluR-A-independent mechanism, by which the associative strength of spatial locations can be increased (and/or decreased) gradually over many trials, and which presumably underlies spatial reference memory acquisition during tasks such as the Morris watermaze or the radial maze (Zamanillo et al.
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The MeO CFO phen yl group was then
2021-09-17

The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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The significance of A and
2021-09-17

The significance of Aβ and tau as therapeutic targets is not only derived from pathological evidence of postmortem brain but also from biochemical analysis of cultured human neurons. This is largely based on the induced pluripotent stem cell (iPSC) technology that has been established to study Aβ, t
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br FXR expression in normal intestine and cancer Of
2021-09-17

FXR PMX 205 in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al., 2013, Kemper et al., 2009
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apoptosis inducer br Material and methods br
2021-09-17

Material and methods Results Discussion Propofol is commonly used in operation rooms or intensive care units (ICUs) for critically ill patients. Various clinical trials have demonstrated that the antioxidant, anti-inflammatory, and free-radical-scavenging properties of propofol can provide
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Michiel S van der Heijden
2021-09-17

Michiel S. van der Heijden had full access to all acetylcholine receptor data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven.
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Consistent with our gene profiling analyses showing
2021-09-17

Consistent with our gene-profiling analyses showing that genes involved in mutual compensation of EGFR or integrin/FAK were significantly downregulated by Tinagl1 overexpression, treatment with r-Tinagl1 inhibited the activation of EGFR and FAK in vitro, and phenocopied the combined inhibition of in
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In enzyme assays it is
2021-09-17

In enzyme assays, it is convenient to quantify the product formed in the enzyme reaction, where a decrease in the concentration of product indicates enzyme inhibition [35], [36], [37], [38]. In the present study, substrates were carefully chosen so that they are specific to each enzyme. Known natura
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Neuropathic pain NP is a chronic pain
2021-09-17

Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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PKC does not however directly stimulate
2021-09-17

PKC does not, however, directly stimulate secretion by initiating calcium influx into the cell [51]. Work from multiple groups measuring calcium currents has shown that PMA alone or coupled with glucose does not modulate intracellular calcium influx [34], [51], [52], [53]. Instead of contributing to
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Methods br Results br Discussion SV
2021-09-17

Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t
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