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Studies of human and mouse GPR as ascertained
2022-01-03

Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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Active compounds and were further
2022-01-03

Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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In conclusion we demonstrate for the first time
2022-01-03

In conclusion, we demonstrate, for the first time, that histamine plays a key role in regulating astrocyte function and gliotransmitter release, and we now must re-consider the roles of monoamine neurotransmitters in brain function in the context of astrocyte signalling. Further in vivo studies will
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The following are the supplementary data related to this
2021-12-31

The following are the supplementary data related to this article. Transparency Document Acknowledgements Introduction Nitric oxide (NO) is an important signaling molecule mediating several physiological functions including vasodilation, platelet anti-aggregation, inhibition of interstitial
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To further investigate the possible
2021-12-31

To further investigate the possible interaction of L1 with β1-sGC, a protein-ligand docking experiment was performed. Calculations were carried out with the program GOLD (version 5.2) [18], [34] and performed with the chemPLP scoring function [19], [34]. The ten lowest energy solutions presented a r
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Decreasing GSK activity has therapeutic benefits in animal
2021-12-31

Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic Imipenem injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregulating Aβ cle
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The compounds described in this
2021-12-31

The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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In recent large clinical studies AIM HIGH and HPS THRIVE
2021-12-31

In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic Edoxaban to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secondary analys
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br Results br Discussion The twin
2021-12-31

Results Discussion The twin-cysteine motif is an evolutionary conserved motif in all primate lentiviruses except HIV-1 and some strains of SIVcpz according to sequence analysis (Bohl et al., 2013). It is assumed that only those SIVcpz which have lost the twin-cysteines successfully evolved to
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Acknowledgements This work is partially supported by the
2021-12-31

Acknowledgements This work is partially supported by the Natural Science Foundation of China(81273353), and the National Science & Technology Key Projects of China (2009ZX09103-085). Glyoxalase I (GLO I) is a key enzyme in the pathways leading to glutathione (GSH)-mediated detoxification of meth
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This work was supported by the National
2021-12-31

This work was supported by the National Natural Science Foundation of China (Grants 81471101 and 81870852), the Natural Science Foundation of Jiangsu Province (Grant BK20181146), the Natural Science Foundation of the Jiangsu Higher Education Institutions of China (Grants 18KJA320007 and 17KJB320018)
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Although encoded by a single gene GR displays
2021-12-31

Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific
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Sulindac synthesis Natural product based drug discovery can
2021-12-30

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in Sulindac synthesis binding assays, we used molecular modeling to predict how well these com
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br Introduction Stroke is the second
2021-12-30

Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A
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br Introduction The coronary vasculature is
2021-12-30

Introduction The coronary vasculature is required for supplying oxygenated blood to the cardiac muscle. Proper coronary blood circulation is essential for embryonic and adult cardiac tissue homeostasis. Defects associated with the coronary function leads to myocardial ischemia, infarction, and he
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