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br EphB as a therapeutic
2020-06-30
EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system
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Considering these reports and with
2020-06-30
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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br Activatable bioorthogonal reactions reagents br Cycloprop
2020-06-30
Activatable bioorthogonal reactions/reagents Cyclopropenes as bioorthogonal reagents for IEDDA substrates Cyclopropenes have become popular bioorthogonal reagents due to their small size, inertness to biological nucleophiles, ability to be genetically encoded (Yu et al., 2012), and participati
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In vasculature NADPH oxidases NOXs are the main
2020-06-30
In vasculature, NADPH oxidases (NOXs) are the main sources of O2− generation that involve in the transfer of electrons to molecular oxygen. Endothelin-1 [25] and thromboxane A2 [26] were reported to induce eNOS uncoupling via upregulation of NOXs. Additionally, inhibition of p47 phox, a subunit of N
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In the previous study glutamyl endopeptidase
2020-06-30
In the previous study glutamyl endopeptidase of B. intermedius has been reported to be distributed in the Octreotide acetate of B. intermedius as follows: 90% of synthesized enzyme has been detected in the culture liquid, 9.3% of glutamyl endopeptidase—in the fraction of membrane proteins [20]. The
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Family and twin studies have
2020-06-30
Family and twin studies have estimated the heritability of obesity to be between 40 and 70% [5], [6], [7]. However, all known risk variants can only account for ∼3% of the variance in BMI [8], [9]. Therefore, alternate methods are needed to identify additional risk factors. In recent decades, Drosop
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Previous synthetic lethal screening efforts Cox et al have
2020-06-30
Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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Because flavonoids are widely considered
2020-06-30
Because flavonoids are widely considered to contribute to health benefits in humans, including anti-inflammatory, antibacterial, antiviral, anticancer, antiplatelet properties, and free radical scavenging capacity (Xiao et al., 2011), efforts have frequently been made to increase their bioavailabili
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Steady state mRNA levels of CYP A isoforms were
2020-06-30
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional activ
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Our results indicate that C
2020-06-30
Our results indicate that C75-CoA is formed in the hypothalamus following stereotaxic injection of C75. Inhibition of hypothalamic CPT1 by C75-CoA in vivo, as seen in our experiments, is independent of the putative inhibition by malonyl-CoA, which may be formed after the action of C75 either on FAS
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There have been two reports of
2020-06-29
There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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The data presented above clearly
2020-06-29
The data presented above clearly indicate an important role of eIF4E for the nucleocytoplasmic transport of the human iNOS mRNA. To analyze the sequence elements of the iNOS mRNA that are important for this eIF4E-mediated transport we performed transient transfection experiments using constructs con
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It is well known that corticotropin releasing factor CRF
2020-06-29
It is well-known that corticotropin-releasing factor (CRF) exerts its biological functions through binding to type-1 (CRF1) and/or type-2 (CRF2) receptors. Several clinical evidences suggest the association of a high level of CRF and the onset of anxiety and depressive disorders.2, 3, 4, 5, 6, 7 Si
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15-deoxy-Δ-12,14-Prostaglandin J2 In order to validate the A
2020-06-29
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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The contradictory effects exerted by metals were
2020-06-29
The contradictory effects exerted by metals were reviewed by Nunes (2011) that stated that the concentration and the species of metal can cause specific effects in ChE activity. Being environmentally exposed, the organism can accumulate metals in tissues, increasing their concentrations. Some author
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