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It is known that microglial function
2021-09-17

It is known that microglial function and morphology are closely related [20], but no studies have addressed whether neuroinflammation induced by alcohol might modify microglial SMI-4a (i.e. morphology, neuroimmunochemical phenotype) through an eCB-dependent mechanism. Since this alcohol-induced mic
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br Results br Discussion Impaired
2021-09-17

Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p
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S1RA A small number of patients had accessory integrase
2021-09-17

A small number of patients (11%) had accessory integrase mutations (E157Q, G163R, L74IM, and/or V151I) that confer potential or low-level resistance and generally only when they occur in combination with other high/intermediate level resistance mutations. This is a somewhat higher incidence than tha
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The histamine H receptor H R
2021-09-16

The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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A nitric oxide donor glyceryl
2021-09-16

A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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Financial nonfinancial disclosures The authors
2021-09-16

Financial/nonfinancial disclosures: The authors have reported to CHEST the following: M. J. A. has received investigator-initiated grants from Pfizer and Boehringer Ingelheim for unrelated research. None declared (X. D., S. C. D., G. B., N. T. W., J. L. P., J. H., B. E., A. J. L., J. A. B., C. S., C
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A general synthetic pathway to these tricyclic structures
2021-09-16

A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy
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Based on the results of compound appeared to have the
2021-09-16

Based on the results of , Galanthamine mg appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while analogs and were
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Our supF forward mutation assay revealed for the
2021-09-16

Our supF forward mutation assay revealed, for the first time, that 5OHU predominantly induced the C→T mutation in human cells. The mechanism underlying the induction of the C→T mutation in human cells by 5OHU remains unclear, however, the finding that 5OHU predominantly induced the C→T mutation was
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br Materials and methods br Results br
2021-09-16

Materials and methods Results Discussion DNA repair pathways have evolved for a long time to act independently of one another. However, over the past decade several overlaps and crosstalks between these pathways were identified, showing that the DNA repair system is more complex than previo
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To this end we evaluated novel D analogs for selectivity
2021-09-16

To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell Salmeterol xinafoate receptor systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursor
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The LBD experiences a large scale conformational transition
2021-09-16

The LBD experiences a large-scale conformational transition between open and closed states upon agonist binding within the cleft separating the two lobes of the domain. The upper lobe (Lobe 1, also called D1) is connected to the ATD, and the lower lobe (Lobe 2, also called D2) is connected to the TM
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To get a broader view of
2021-09-16

To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat X-NeuNAc australia and confirm the inhibition of this i
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br Declaration of interest br
2021-09-16

Declaration of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 31471615), the Introduction of Talent Research Start-up Fund of Anhui Polytechnic University (No. 2017YQQ017) and the Pre-research Project of National Natural Sc
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In the present study we set out to
2021-09-16

In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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