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EP receptor is known to
2021-05-10
EP4 receptor is known to mediate the protective effect of PGE2 on the respiratory, gastrointestinal and glomerular epithelial lining (Aoudjit et al, 2006, Kabashima et al, 2002, Schmidt et al, 2011). In this study, the expression of asEP4 in the gills was limited to the epithelial lining suggesting
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PI K is a lipid kinase and
2021-05-10
PI3K is a lipid kinase and generates phosphatidylinositol-(3,4,5)-trisphosphate, which is a second messenger critical for the translocation of Akt to the cytoplasmic membrane. The phosphorylation of Ser473 Akt is important in the cell survival by regulating the eNOS among other targets (Dimmeler et
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br A major physiological action of ET
2021-05-10
A major physiological action of ET-1 is to function as one of the most powerful vasoconstrictors of human blood vessels. As such, ET-1 plays a major role in regulating vascular function in all organ systems, including the kidney (Fig. 1). As in other vessels, ET-1 is thought to be released from e
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Our recent discovery M P
2021-05-10
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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In conclusion we developed a new
2021-05-10
In conclusion, we developed a new CysLT1 and CysLT2 receptors-mediated anaphylaxis guinea pig model that can be useful for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. In addition, we have shown that the dual CysLT1/2 receptor antagonist ONO-6950 can exert protective effect agai
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Redundancy of tumor promoting signaling pathways is one of
2021-05-10
Redundancy of tumor promoting signaling pathways is one of the mechanisms that prevent a lasting effect of targeted therapies, as has been demonstrated by the growing number of alternative pathways that confer resistance to EGFR-targeted therapies [3]. We show here that CSF-1R can, at least partiall
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Regarding the mechanism of action of CRF several studies
2021-05-10
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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The use of inhibitors clearly has its caveats and
2021-05-08
The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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The in vitro cytotoxicity of the prodrugs was
2021-05-08
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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br Disclosures br Introduction The
2021-05-08
Disclosures Introduction The presence of anti-viral T-cell immunity is crucial for effective and sustained protection against Cytomegalovirus (CMV) following allogeneic stem cell transplantation (alloSCT) [1]. In vitro and in vivo T-cell depletion (TCD) via addition of the anti-CD52 monoclonal
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br Allosteric inhibitors In general candidate drugs
2021-05-08
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Introduction Angiotensin II Ang II
2021-05-08
Introduction Angiotensin II (Ang II) and Endothelin 1 (ET-1) are potent vasoconstrictive peptides recognized as key players in many cardiovascular diseases [1]. Cardiac hypertrophy, ischemic arrhythmia, and stroke have been associated to an overstimulation of the angiotensin II type 1 (AT1) recepto
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Many researchers studied the experimental
2021-05-08
Many researchers studied the experimental investigation of RHA in cement enhances the strength and durability of the concrete [9], [10], [11], [12]. It is most important that concrete must withstand its strength even after it is being exposed to any corrosive environment over a period of time. In ad
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ERRGO mice exhibited increased oxygen consumption decreased
2021-05-08
ERRGO mice exhibited increased oxygen consumption, decreased RER, high running endurance, and resistance to diet-induced weight gain. These changes are physiological hallmarks of increased aerobic capacity in mice and are a direct consequence of engineering highly oxidative and vascularized muscle b
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br Discussion The N terminal domain of DDRs has long
2021-05-08
Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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