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In addition to the above
2022-10-25

In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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br Disclosure statement br Acknowledgements
2022-10-25

Disclosure statement Acknowledgements The work was supported by the National Science Foundation of China (Nos. 81273526, 81473268) and Natural Science Foundation of Colleges and Universities (Nos. KJ2017A197). What is already known What this article adds Introduction Sevoflurane is o
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The identification of novel kinase inhibitor scaffolds is hi
2022-10-25

The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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Although the LB domains of mGlu
2022-10-25

Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V
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A disruption of lung barrier
2022-10-25

A disruption of lung barrier function caused by PM2.5 has been observed in our experiments; however the underlying mechanism has not been investigated. Zhao et al. (2018) reported that PM2.5 down-regulated the expression levels of tight junction (TJ) proteins and resulted in nasal epithelial barrier
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Based on the results of studies done to
2022-10-25

Based on the results of studies done to-date, there are three characteristics that make a letrozole-based protocol attractive for use in cattle: 1) it is steroid-free, 2) it is cost-effective and requires a shorter time and fewer animal handlings than conventional methods (Table 1), and 3) it may ha
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As an internal control this study validated many
2022-10-25

As an internal control, this study validated many of the known associations between GATA3 and predictive markers. GATA3 was shown to be associated with ER and PR, which are both well-known correlations. GATA3 was also negatively correlated with nuclear grade, which is consistent with our knowledge o
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HBC br Conclusions br Transparency document
2022-10-25

Conclusions Transparency document Acknowledgements This work was supported by a grant from the European Commission FP6 “Neuroprion” – Network of Excellence and Royal Veterinary College Bioveterinary science research project funding. We thank Professor Alun Williams (Cambridge University) fo
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The preferential expression of ALOX B in human macrophages m
2022-10-24

The preferential expression of ALOX15B in human macrophages may explain why human genetic studies investigating the association of ALOX15 with cardiovascular disease did not show consistent results. Two rare functional polymorphisms have been characterized in the ALOX15 gene, which leads to increase
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br Adenosine receptors and innate immunity Monocytes and
2022-10-24

Adenosine receptors and innate immunity Monocytes and macrophages. All four adenosine receptor subtypes are expressed on monocytes and macrophages, and their levels and function undergo significant changes during the maturation of macrophages from monocytes. Indeed, quiescent monocytes are charac
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Until now the molecular interactions of Tmod or Lmod
2022-10-24

Until now, the molecular interactions of Tmod or Lmod with LFM-A13 had been assessed in pyrene-actin polymerization assays [13], [23], [27], [28], [44], [45] or directly measured using non-denaturing polyacrylamide gel-electrophoresis (for Tmod isoforms only [23]), ITC (for Tmod1 and Lmod2) [43], [4
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Having taken a step back from affinity to gain
2022-10-22

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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PF also a dual Aurora
2022-10-22

PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly T16Ainh - A01 for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was de
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The resolution cocrystal structure of
2022-10-22

The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of
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br Resection of DNA ends The highly conserved
2022-10-22

Resection of DNA ends The highly conserved MRN/MRX complex (Mre11-Rad50-Nbs1 in metazoan; Mre11-Rad50-Xrs2 in yeast) and the Ku70/Ku80 heterodimer (hereafter referred to as Ku) are the first protein complexes to be recruited at DSBs [6]. The presence of Ku and MRN/MRX mediates the recruitment of
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