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To investigate an involvement of GPR and
2022-06-07
To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) caudatin mg were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, while n
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br Conclusions Our in vitro and
2022-06-07
Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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Combination inhibitors of FAAH TRPV and or COX may
2022-06-07
Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had grea
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Trifluoromethyl ketones and fluorophosphates were the first
2022-06-07
Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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Tylophora atrofolliculata is a centuries used folk
2022-06-07
Tylophora atrofolliculata is a centuries-used folk medicine for the treatment of rheumatism in China (Jiangsu New Medical College, 1977). One group of its bioactive components is phenanthroindolizidine alkaloids, which have been demonstrated as lead compounds of anti-tumor agents in our previous stu
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Most studies of HIF have focused
2022-06-07
Most studies of HIF-1α have focused on its transcriptional activity-dependent functions. However, our results indicate that the oxidative stress-related effects of mtHIF-1α occur independently of its translocation to the nucleus and do not require its transcriptional activity. In fact, several studi
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Anti apoptotic Bcl proteins have become attractive targets
2022-06-07
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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A more quantitative view of
2022-06-07
A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing or
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Modulation of the cannabinoid system has been reported to
2022-06-07
Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a
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br Introduction Methylglyoxal MG is a highly reactive dicarb
2022-06-06
Introduction Methylglyoxal (MG) is a highly reactive dicarbonyl metabolite formed in cells mainly by the spontaneous degradation of triose phosphates, glyceraldehyde-3-phosphate, and dihydroxyacetone phosphate (Rabbani and Thornalley, 2012). It exists in a wide range of organisms, including proto
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berbamine In this study we examined
2022-06-06
In this study, we examined whether zebrafish ionocytes might also share other types of similarity in transport function with kidney cells. In addition to ion transport, mammalian kidney berbamine also play key roles in xenobiotic elimination, through the action of ATP-Binding Cassette (ABC) transpor
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br Conclusion Until recently astrocytes were recognized sole
2022-06-06
Conclusion Until recently, astrocytes were recognized solely for their maintenance role in the regulation of Study Interventions homeostasis. Nowadays, this idea has changed, it is clear that these cells play a crucial role in the regulation of neuronal activity and signal transmission. In parti
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Finally it is possible that
2022-06-06
Finally, it is possible that the increase in the number of EAAT-3-labelled cells in the DG at PD 60, when compared with the control and experimental animals at PD 14, is associated with natural changes in the number of neurons present during the postnatal development of the hippocampus (41, 42) and,
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In the present study five Glu substituted analogues of
2022-06-06
In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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It was recently reported that aged
2022-06-06
It was recently reported that aged GHSR−/− mice, in addition to showing alterations in meal pattern microstructure, exhibit NPY and AgRP mRNA upregulation in the ARC [56]. After an overnight fast, our animals exhibited a similar pattern of upregulated NPY and AgRP mRNA expression. Given that GHSR1a
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