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GLP signaling mediates important renal functions as suggeste
2021-05-11
GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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Approximately of the etamicastat dose was
2021-05-11
Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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br The major regulator of radiation sensitivity
2021-05-11
The major regulator of radiation sensitivity Tumor cell resistance to radiation is a big issue for radiation therapy, and a major concern of radiation oncologist. Understanding the regulation mechanism of radiation sensitivity is still a research hotspot. Increased sensitivity to ionizing radiati
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Several authors have been pursuing
2021-05-11
Several authors have been pursuing the aim of finding good performing organic solvent compatible adsorbers useful in the context of API purification [[10], [11], [12], [13], 22, 23]. For sulfonate GTIs, scavenging nucleophilic resins [22, 23] or molecular imprinted polymers (MIPs) [10] have been exp
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To compare glucose metabolism via oxidative phosphorylation
2021-05-11
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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br Acknowledgments br Casein kinases CK
2021-05-10
Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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The N B method has the overall advantage that
2021-05-10
The N&B method has the overall advantage that it is not restricted to certain dyes specific for energy transfer [55], and is also able to detect higher order receptor Balaglitazone receptor on the focal point in living cells. Conclusion The N&B method has shown to be a powerful tool to locate a
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The compounds listed in Table Table Table Table Table were
2021-05-10
The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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Among RAS mutant tumors analyzed we found that the efficacy
2021-05-10
Among RAS mutant tumors analyzed, we found that the efficacy of either the SHP2 inhibitor SHP099, or combined MEK and SHP2 inhibition was best in those expressing RAS mutations at G12 (Figure 7B). Recent studies revealed that cellular RAS(G12C) activity depends on RTK-mediated nucleotide exchange, a
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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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