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In conclusion we have demonstrated that diaryl
2024-07-20
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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br Abbreviations br Acknowledgements This work was supported
2024-07-20
Abbreviations Acknowledgements This work was supported by grants from the National Institutes of Health (R01GM114168) and the Office of Naval Research (N000141210773) awarded to J.C·H and National Cancer Institute (5P30CA16059) Cancer Center Support Grant in support of Massey Cancer Center Pro
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We subsequently performed immunohistochemistry on sections o
2024-07-20
We subsequently performed immunohistochemistry on sections obtained from mice at 16 weeks after surgery. Type II collagen expression was detected in all articular cartilage zones, but was weak in the upper zone in the vehicle-treated group. MMP-13 and type X collagen expression were increased in the
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According to the present observations
2024-07-20
According to the present observations, the Ampkα1 isoform promotes AP-1 transcriptional activity and thereby fosters live dead stain flow cytometry of AP-1 target genes in cardiomyocytes via activation of Pkcζ. The transcription factor AP-1 plays a decisive role during cardiac remodeling [24], [25]
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Plant pathogenic fungi have caused a lot of
2024-07-20
Plant pathogenic fungi have caused a lot of economic losses to agricultural production worldwide every year. It is necessary to develop an bio-sourced antifungal agent for agricultural use. Many researches have shown that the antifungal activity of quaternized chitosan derivatives is mainly affected
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br Angiotensin receptor neprilysin inhibitors
2024-07-20
Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu
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We next considered the effect of
2024-07-19
We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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AKT activity is also self limiting through
2024-07-19
AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa
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Recently several groups including ours have
2024-07-19
Recently, several groups, including ours, have started to use the C. elegans multi-dendritic PVD neurons as a model system to dissect the molecular mechanisms of dendrite development. During larval development, PVD elaborates complex and stereotyped dendritic arbors by sequentially adding primary (1
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Although the mechanisms of APP secretion are well characteri
2024-07-19
Although the mechanisms of APP secretion are well characterised (for review see Ref. [1]), production of soluble AChE species is less well understood although we have reported that a metalloproteinase can shed AChE similarly to APP [16], [17]. Recently it has also been demonstrated that cellular pre
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Although CP has been an important research subject
2024-07-19
Although CP has been an important research subject in the field of antigen processing and presentation, the mechanisms of presentation of intracellular FITC, Fluorescein isothiocyanate by MHC II received considerably less attention. Interestingly, pioneering work by the Münz laboratory has pointed
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The known crystal structures of class C GPCR VFTs
2024-07-19
The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S
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Thus phosphorylation of p was used to measure the
2024-07-19
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc A-1155463 expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Res
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Additionally we used the predicted Cyp a b
2024-07-19
Additionally, we used the predicted Cyp19a1b amino cas9 size sequence from a number of bony fish species to infer their genetic relatedness and found that R. quelen occupies an ancient position within the Siluriformes group. A phylogenetic tree was constructed and it included both full-length and p
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Using this cheese mimicking matrix we screened the antifunga
2024-07-18
Using this cheese-mimicking matrix, we screened the antifungal activity of 44 LAB fermented milk-based products and 23 LAB isolates used as protective cultures against 4 fungal targets. The LAB were obtained from the culture collections of CIRM-BIA (Centre International de Ressources Microbienne-Bac
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