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The present study has several limitations First the
2024-04-02
The present study has several limitations. First, the results were obtained using RAW264.7 cells, which are derived from BALB/c mice infected with the Abelson leukemia virus (Raschke et al., 1978). However, these cells, which are a commonly used mouse macrophage cell line, show properties similar to
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Thirty six of the analogs synthesized showed ATX inhibition
2024-04-02
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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br Results and discussion br Conclusion In summary
2024-04-02
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic calpain inhibitor group extending from the C-3 position of the aniline and substitu
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br Experimental Procedures Additional information can be fou
2024-04-02
Experimental Procedures Additional information can be found in Supplemental Experimental Procedures. Author Contributions Acknowledgments We thank all members of Lab of Health Chemistry for helpful discussions. This work was supported by Grant-in-Aid for Scientific Research (KAKENHI) from
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Calcineurin has been established to be a ubiquitous
2024-04-02
Calcineurin has been established to be a ubiquitous Ca2+-activated serine phosphatase in the nervous system (Pyrzynska et al., 2001). It has been reported that the activation of calcineurin protects aromatase from autophagy-mediated protein degradation, implying that calcineurin-dependent dephosphor
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In addition to attracting immune cells to the
2024-04-02
In addition to attracting immune cells to the site of injury, ROS also participate in proliferative responses during compensatory proliferation and regeneration. In Xenopus tadpoles, tail amputation induces sustained production of ROS over the span of regeneration, and decreasing ROS levels, especia
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Introduction Hepatocellular carcinoma HCC is one of the most
2024-04-02
Introduction Hepatocellular carcinoma (HCC) is one of the most difficult cancers to treat, and it threatens human health severely [1]. Although various interventions, including surgical operation, radiofrequency ablation, and chemotherapy, have been endorsed, the prognosis of HCC patients remains p
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br Author contributions br Funding This work was
2024-04-01
Author contributions Funding This work was supported by the Czech Science Foundation, project no. 14-16220S. Additional support was provided by NIH R01CA117907 grant awarded to J.M.E. Conflict of interest Introduction The dioxin-like family includes polyhalogenated aromatic hydrocarbons
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With one exception all receptors for dopamine
2024-04-01
With one exception, all receptors for dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT), and norepinephrine are metabotropic receptors. The five metabotropic DA receptors (D1–D5) in the CNS are involved in motivation, pleasure, cognition, learning, memory, fine motor control, and modulate neuroen
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In summary the different types of interstitial cells
2024-04-01
In summary, the different types of interstitial cells found in the current study are illustrated in Fig. 7A (see legend for further details), which is suggestive of a heterogeneous complex network of interstitial cells communicating with each other. The possible signaling pathways involving this int
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br Discussion With recently improved understanding of the ro
2024-04-01
Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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The potential use of derivatives
2024-04-01
The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore
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The hypothalamic pituitary adrenal HPA axis
2024-04-01
The hypothalamic-pituitary-adrenal (HPA) axis is a neuroendocrine system that is central to regulating responses to stress (Palazidou, 2012). In older persons, a high dysfunction of the HPA axis is observed (Otte et al., 2005) which may be enhanced by stimulatory effects of genes involved in the axi
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In conclusion we have designed
2024-04-01
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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br Materials and methods br Results br Discussion Recent stu
2024-04-01
Materials and methods Results Discussion Recent studies have highlighted Luciferase Reporter Assay Kit and autophagy as novel targets for the treatment of liver fibrosis [7,14]. In this study, we demonstrated that catalpol protected the rat liver from CCl4-caused injury and fibrogenesis in
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