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Small kinase inhibitors have been developed to block AXL by
2023-10-10
Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha
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The synthetic route for the aminobenzoxazole scaffold with
2023-10-10
The synthetic route for the aminobenzoxazole scaffold with a solvent accessible moiety is described in . Nitration of methoxyphenol and subsequent hydrogenation of the resulting nitro 91 5 australia afforded compound . Aminobenzoxazole was formed by the reaction of compound with BrCN in EtOH. The
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It has been shown that ACLY is localized
2023-10-10
It has been shown that ACLY is localized to not only the cytoplasm but also the nucleus. Nuclear ACLY may supply acetyl-CoA for histone acetylation, leading to global regulation of the gene expression [16], [18]. We previously reported that AZ2 is also localized to both the cytoplasm and nucleus whe
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L-Homopropargyl Glycine exemplifies three of the compounds i
2023-10-10
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC L-Homopropargyl Glycine as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradat
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In the pituitary of R quelen mRNA levels of cyp
2023-10-10
In the pituitary of R. quelen mRNA levels of cyp19a1b were found to be higher in males than females, suggesting a sex-specific function, and perhaps a local action to regulate gonadotropins or other pituitary hormone secretion (Olivereau and Callard, 1985; Zhang et al., 2014). Interestingly, the hig
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There is limited information regarding hyperargininemia
2023-10-10
There is limited information regarding hyperargininemia incidence or prevalence. Reports of incidence vary by an order of magnitude: 0.5 to 5.0 per million [5], [6]. A relatively large U.S. study estimated 1.1 cases per million births [7], but it used an indirect methodology that introduces uncertai
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Using this cheese mimicking matrix we screened the antifunga
2023-10-10
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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In humans the superior safety profile
2023-10-10
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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Incubation of the aortic segments of
2023-10-10
Incubation of the aortic segments of rats with indomethacin significantly decreased the vasoconstrictor response to Phe but only in HgCl2-treated group (Fig. 9A,B), as indicated by dAUC values (Fig. 9E). Co-treatment with losartan once again proved to be effective and prevented the increased partici
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First the complete canonical brain
2023-10-10
First, the complete canonical brain original RAS (Angiotensinogen, Renin, Angiotensin I, Angiotensin Converting Enzyme (ACE), Angiotensin II) has not been conclusively identified in any specific cell type within the brain [1]. Validated evidence for the presence of brain Angiotensinogen and ACE was
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Ultracentrifugation of AD brain was reported to remove of
2023-10-10
Ultracentrifugation of AD ck1 inhibitor was reported to remove >99.95% of Aβ, while only reducing seeding capacity by 70% (Langer et al., 2011). This suggests that the most potent seeding Aβ species are relatively small soluble oligomers rather than larger insoluble fibrils. It was also noted that
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bet bromodomain PF is orally bioavailable and has appropriat
2023-10-10
PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) br Exp
2023-10-10
Experimental Procedures Acknowledgments Introduction Cellular and molecular mechanisms underlying synaptic plasticity in the Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) are thought to be involved in memory acquisition. Synaptic plasticity is categorised into two main types, long-
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br Discussion Missense mutations transversions of
2023-10-10
Discussion Missense mutations (transversions) of the first nucleotide of the phenylalanine phalloidin at position 1174 (F1174) of the anaplastic lymphoma kinase gene can result in substitutions to leucine or valine (F1174L/V) while missense mutation (transversion) of the second nucleotide of the
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Our previous study revealed expression of AhR in human
2023-10-10
Our previous study revealed expression of AhR in human parotid gland in cytoplasm of striated duct CCT241533 hydrochloride sale (Drozdzik, Kowalczyk, Urasińska, & Kurzawski, 2013). In a further study we observed regulation of AhR expression and function by its specific inducer, i.e. 2,3,7,8-tetrachl
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