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Another topic for research will be the combination
2023-08-17
Another topic for research will be the combination of other cytotoxic agents with Aurora kinase inhibitors. Particularly interesting might be the combination of Aurora kinase inhibitors and agents that depend on the spindle checkpoint for their activity, such as the taxanes, given the importance of
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Here we report discovery of highly selective pan Aurora kina
2023-08-17
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of 69 9 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To identif
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In addition to drawing attention to Ser of
2023-08-17
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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On the other hand there were only
2023-08-17
On the other hand, there were only a few cases that expressed DA2R in our study. Additionally, in the cases whose ACTH-secreting pituitary adenomas expressed DA2R, the ratio of positive staining Ergosterol mg was very low. This suggests that dopamine agonists may be less effective in canine Cushing'
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The growth of cancer can control by
2023-08-17
The growth of cancer can control by inhibiting the rate of cell proliferation or increasing the rate of selective apoptosis and effectiveness of anticancer agents varies according to genetic constitution of cancer. Hence, we investigated the anticancer activity of arginase against different kinds of
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Therefore we have further investigated the anti oxidant
2023-08-16
Therefore, we have further investigated the anti-oxidant activity of isogarcinol in vitro by measuring the scavenging of 2,2′-diphenyl-1-1picrylhydrazyl (DPPH) and 2,2′-azino-bia (3-ethylben-zothiazoline-6-sulphonicacid) (ABTS), and determining its reducing power and ability to prevent lipid peroxid
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A key function of the reference AFST would be to
2023-08-16
A key function of the reference AFST would be to detect fungal resistance, i.e. to determine which antifungal agents are likely to be clinically inactive [2]. To this end, the epidemiological cut-off value, defined as ‘the upper end of the wild-type (WT) or beginning of the non-wild-type (NWT) MIC d
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Of the cardiovascular studies involving ARBs reported renal
2023-08-16
Of the cardiovascular studies involving ARBs, 3 reported renal outcomes. In the Losartan Intervention For Endpoint study, albuminuria was observed less frequently in the losartan than in the atenolol arm (7% vs. 13%; p=0.002) (5). In the Candesartan Antihypertensive Survival Evaluation in Japan tria
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In conclusion we have shown that mGlu receptors negatively
2023-08-16
In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, prostaglandin synthase tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of norad
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Carteolol HCl Application of the broad acting HTR antagonist
2023-08-16
Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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By applying each external load to
2023-08-16
By applying each external load to the G-actin molecule, and measuring the elongation of the molecule, we computed force-displacement curves. The force versus displacement curve can be used to evaluate the tensile stiffness of the G-actin from a linear regression analysis. Followed by statistical ana
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We have expressed the ECDs of
2023-08-16
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydrop
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Several dehidropregnenolone derivatives functionalized at C
2023-08-16
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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To identify the kinase s mediating
2023-08-16
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with palmitic acid specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck) containing 194
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br Concluding Remarks and Future Perspectives Fluorescent an
2023-08-15
Concluding Remarks and Future Perspectives Fluorescent SCH772984 TFA have helped researchers to elucidate antibiotic MOA and off-target interactions, to screen for new antibiotics, to detect antibiotics in the environment, to track antibiotic uptake throughout cells and organisms, and to detect b
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