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As mentioned above variation of the A ring
2024-06-14
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to PTC209 HBr (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparable in
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In this paper we describe the formation of a structure
2024-06-14
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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br Materials and methods br Results br Discussion Recent
2024-06-14
Materials and methods Results Discussion Recent studies have highlighted Metaphit 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 vivo and in vitro fo
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As summarized in Fig autophagy up
2024-06-14
As summarized in Fig. 1, autophagy up-regulation in terms of Beclin 1 induction, increase of LC3 II and p62 down-regulation were observed between 24 and 72 h of cell incubation, this coinciding with the end of the period 27-OH caused slight reduction of cell viability and proliferation as previously
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Aurora A and B are
2024-06-14
Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for t
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Inactivation of the proton pump
2024-06-14
Inactivation of the proton pump comes with luminal alkalinization of the targeted vesicles such as lysosomes (Fig. 2b). Lysosome pH can also be raised stoichiometrically by addition of a membrane-permeable weak Neurotensin such as methylamine or chloroquine which accumulates in its protonated, non-m
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Upregulation of ACLY is common in many
2024-06-14
Upregulation of ACLY is common in many cancers (Kuhajda, 2000, Milgraum et al., 1997, Swinnen et al., 2004, Yahagi et al., 2005). This is in part due to the transcriptional activation by SREBP-1 resulting from the activation of the PI3K/AKT pathway in cancers (Kim et al., 2010, Nadler et al., 2001,
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Currently NSAIDs which achieve antineoplastic actions mainly
2024-06-13
Currently, NSAIDs which achieve antineoplastic actions mainly through apoptosis are emerging choice in chemotherapy. Their antineoplastic effects were demonstrated before in tumor-bearing models [5], [6], [7]. Through in vitro cell models, we identified an indomethacin-activation of ceramide/PP2A/Ak
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We further conducted stratified analyses to observe
2024-06-13
We further conducted stratified analyses to observe changes in enzyme levels across the periods by subgroups. Fig. 1 shows the changes in GPx levels by subgroups of age, sex, and smoking status. In all participants, GPx levels decreased when air pollution levels declined but increased after the Olym
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br Epidemiology br Genetics The dominantly inherited PrP
2024-06-13
Epidemiology Genetics The dominantly inherited PrP cerebral amyloidoses are genetically transmitted with a penetrance of almost 100%. Early linkage analysis studies helped to established the relationship between GSS and mutations in the PRNP gene. PRNP is located on the short arm of chromosome
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In humans the superior safety profile
2024-06-13
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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Since at least prospective cohort
2024-06-13
Since 2005, at least 14 prospective cohort studies have been conducted to clarify inconsistencies in the field, ten of which suggested a direct correlation between antibiotic use and atopy or wheezing later in life [51–60], three found no association [61–63], and one found positive association only
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br Conclusions br Funding This work
2024-06-13
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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Maynard et al demonstrated that serum levels
2024-06-13
Maynard et al. [54] demonstrated that serum levels of sFlt-1 were five times higher in pregnant women with PE than in normotensive women; as a consequence, VEGF and PlGF levels were found to be proportionally reduced in these women [54]. The literature confirms that there is a sharp increase in sFlt
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Although little is known about the etiopathogenesis of preec
2024-06-13
Although little is known about the etiopathogenesis of preeclampsia, this syndrome has a major impact on maternal and fetal health worldwide, since it is responsible for 10–15% of maternal deaths [16], [17], preterm births, intrauterine growth restriction (IUGR), and fetal deaths [2]. In developing
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