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simvastin Grapiprant is a selective antagonist for prostagla
2020-11-14
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Another important new result that has expanded the range
2020-11-14
Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f
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Importantly MPO is not only
2020-11-13
Importantly, MPO is not only a marker of cardiovascular disease but also emerges as a critical mediator of vascular inflammatory disease: Liberated MPO binds to the endothelium in a leukocyte-independent manner, is subsequently taken up by the endothelium and transcytoses and accumulates in the sube
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Collectively the results presented here provide new insights
2020-11-13
Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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CSN was initially identified based on the constitutitvely ph
2020-11-13
CSN was initially identified based on the constitutitvely photormophogenic (cop) mutants from Arabidopsis thaliana [48]. csn mutants are Cullin deneddylation-deficient, consequently accumulate neddylated Cullins, and arrest growth shortly after germination [49, 50, 51]. Weak csn mutants have defects
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The differences between ground and transition state
2020-11-13
The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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The first ones class A receptors found as
2020-11-13
The first ones class A receptors found as heterodimers were reported by Gomes et al. (2000), who identified a heteromer constituted by two subtypes of opioid receptors (μ and δ) in heterologous cells. The same year, Ginés et al. (2000) showed the first heteromer composed of two different receptors,
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br General mechanism of NHEJ NHEJ is an
2020-11-13
General mechanism of NHEJ NHEJ is an amazingly versatile pathway that can select specific enzymes which bind to, process, and finally mediate the direct re-ligation of a wide range of DSBs including those that are complex, have incompatible ends, and contain Cy3-dUTP damages [7], [8], [9], [10].
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beta lactamase inhibitor Previous in vitro studies have demo
2020-11-13
Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM beta lactamase inhibito
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In general graphene nanoplatelets have many useful
2020-11-13
In general, graphene nanoplatelets have many useful features for the design of multifunctional composite materials, including excellent electrical and thermal conductivities, considerable weight-saving lightness, and high mechanical strength [26]. Moreover, they are characterized by a high specific
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ABH expression is elevated in prostate carcinomas and has be
2020-11-13
ABH3 expression is elevated in prostate carcinomas and has been referred to as prostate cancer antigen-1 or PCA-1. ABH3/PCA-1 was proposed as a diagnostic marker for prostate cancers, and suggested as a possible therapeutic target [82]. However, the recent studies of ABH2 and ABH3-null mice indicate
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To compare glucose metabolism via
2020-11-13
To compare glucose metabolism via oxidative phosphorylation to that via glycolysis, a bioenergetics plot was constructed (Fig. 3A). In most cells, a decrease in one bioenergetics pathway is compensated by an increase in the other. However, following NAT1 deletion, there was a decrease in both oxidat
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By stratifying EOC cell lines
2020-11-13
By stratifying EOC cell lines according to their EMT stages, we observed a significant higher expression of DDR1 in the epithelial-like cell lines compared to low or undetectable DDR1 in mesenchymal-like cell lines. Similar trend was observed in the tumour samples, with the lowest expression of DDR1
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795 Regarding the mechanism of action of CRF several
2020-11-13
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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Synthetic peptides have proven highly valuable in replicatin
2020-11-12
Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of
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