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Dexamethasone DEX a potent synthetic
2021-03-25
Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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WP1130 Although it is believed that CYP induction
2021-03-25
Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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Acidic substituents showed moderate biochemical activity but
2021-03-25
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic 6063 were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical activi
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There was a measurable worsening but not a
2021-03-24
There was a measurable worsening, but not a statistically significant change in the baseline and follow-up best ear hearing scores, where the mean worsening change was 11.9 dB (95% CI: −1.11–24.86, p-value = 0.070). However, of the 16 patients, 14 (87.5%) were found to have clinically significant wo
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Mouse Cyp a is a homologous
2021-03-24
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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It is interesting to note that Eibinger and colleagues
2021-03-24
It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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We then evaluated in vivo
2021-03-24
We then evaluated in vivo DHODH mRNA Genomic DNA Isolation Kit sale using data from TCGA (Lee, Palm, Grimes, & Ji, 2015). To perform a pan-disease comparison of DHODH expression, log2 TPM expression values were converted to z-scores calculated per patient. Fig. 6 shows that across all 34 diseases (9
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In summary our data show a
2021-03-24
In summary, our data show a novel mechanism: CPD-mediated autoprocessing of C difficile toxins regulates their proinflammatory activities. Thus, our study provides a new understanding of the molecular mechanisms of the pathogenesis of C difficile toxins and insights into designing new therapeutics a
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In this study cell migration in response to
2021-03-24
In this study, cell migration in response to LTD4 exhibited a typical bell-shaped dose-response curve with optimal activity at 10 nM. However, the effect of inhaled CysLTs on airway inflammatory cells in vivo has not been widely reported to date, therefore, the role of CysLTs in the development of a
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In the cytoplasm the ternary CRM cargo
2021-03-24
In the cytoplasm, the ternary CRM1–cargo–RanGTP complex is disassembled by the action of Ran-binding proteins RanBP1/2 and RanGAP. A recent kinetic study showed that the Ran-binding domains (RanBDs) of the cytoplasmic proteins RanBP1 and RanBP2, but not RanGAP, accelerate dissociation of NES from C
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In this study we observed
2021-03-24
In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased PF-00562271 receptor when the sensitization condition was established. Similarly, CRF2 rece
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br Alcohol and the amygdala br Alcohol and the
2021-03-24
Alcohol and the amygdala Alcohol and the CRF1 system Given the marked effects of alcohol on inhibitory neurotransmission in the amygdala and the regulation of amygdalar GABAergic activity by CRF and activity at the CRF1 receptor, the CRF system is a logical site for the actions of alcohol in
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br Conclusions br Source of
2021-03-23
Conclusions Source of financial support or funding This investigation was supported by the University of Utah Study Design and Biostatistics Center, with funding in part from the National Center for Research Resources and the National Center for Advancing Translational Sciences, National Insti
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Finally we have determined for the first time that aromatase
2021-03-23
Finally, we have determined for the first time that aromatase enzyme activity is necessary to observe IGF-1-dependent q vd oph mg receptor activation. Neuroestrogen synthesis has been shown to be important for the maintenance of synaptic spine density in hippocampal slice cultures (Kretz et al., 20
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In our former work our interest was in discovery of
2021-03-23
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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