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br Introduction The cys loop ligand gated ion channels LGICs
2020-01-30

Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri
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The upregulation of PTGS and
2020-01-30

The upregulation of PTGS1 and PTGS2 in late gestation in mares could be linked to the high levels of estrogens produced by the fetoplacental unit. Estrogens are thought to be effective stimulators of prostaglandin production by potentially up regulating PTGS2 expression. Although a recent publicatio
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The imaging and biochemical data presented here
2020-01-29

The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a
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From these and other studies it is
2020-01-29

From these and other studies, it is clear that acriflavine is an interesting casr with pleiotropic anticancer effects [21], [22], [43]. Its past systemic use in the clinical setting as an antibiotic without any major toxicity reported encourages further development of the drug for cancer treatment
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It is interesting to note that Eibinger and
2020-01-29

It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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br Results and discussion br Conclusion In the current
2020-01-29

Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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We have compared the potency of a series of
2020-01-29

We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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Our results suggest that formation of DDR
2020-01-29

Our results suggest that formation of DDR1b clusters may be important for and precede receptor phosphorylation. Indeed, while DDR1b clustering was readily detected (by YFP signal) 30 min after collagen administration, phosphorylated DDR1 species at Y513 (present in the IJXM) were evident after 4 h o
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In the present study we combined activity based
2020-01-29

In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis Nemadectin and leaves, we demonstrate that this sub-class of plant proteases is activated in r
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From the general synthetic route we first
2020-01-29

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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It has been reported that NMDA
2020-01-29

It has been reported that NMDA receptor hypofunction upregulates the expression of immediate early genes in several Caspase-9 Colorimetric Assay Kit regions [39], [40]. Consistent with this finding, we demonstrated that MK-801 increased the number of c-Fos-positive cells in the PVN and PC/RS (Fig.
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Our results also showed that
2020-01-29

Our results also showed that the highest dose of Astressin2-B increased the rewarding effects of cocaine, since non-defeated animals treated with this dose developed CPP with a sub-threshold dose. We monitored the acute effects of 30 µg/kg of Astressin2-B and found an increase of anxiety in the open
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Introduction The first reference to
2020-01-29

Introduction The first reference to a possible involvement of orexins in the effects of drugs of abuse appeared in 2003 and showed that orexigenic peptide neurons respond to the chronic administration of morphine followed by abrupt withdrawal symptoms caused by opioid receptor antagonists (Georgesc
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These cognitive deficits may suggest that
2020-01-29

These cognitive deficits may suggest that cognitive therapy and pharmacotherapy for gambling behavior may ultimately wish to consider genotyping as a means of better targeting treatment approaches. If core cognitive deficits are shown consistently in certain subgroups of gamblers based on genotype,
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The four other mutations S
2020-01-29

The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels
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