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Conclusion Twenty compounds with dinitrobenzoate
2024-04-01

Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5
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NLX a k a F or befiradol
2024-04-01

NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in AZD2932 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has s
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In the current study we provide evidence that enhanced ATX
2024-04-01

In the current study, we provide evidence that enhanced ATX activity correlates well with increased ATX protein concentration during cholestasis and pregnancy (Fig. 1). Hereby we have ruled out the possibility of ATX enzyme activation in these conditions, e.g. by circulating cholephiles. ATX clearan
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br Methods br Results br Discussion Autotaxin has been shown
2024-04-01

Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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Pompe disease is accompanied by the deficiency of
2024-04-01

Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the PEG Virus Precipitation Kit receptor unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This acc
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Aurora A or B selective and pan aurora
2024-04-01

Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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br Conclusion This is the
2024-04-01

Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,
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br Materials and methods br Results br Discussion
2024-04-01

Materials and methods Results Discussion Despite the relative complexity of immunotherapy, such treatment may have an important role, in conjunction with other therapies in the treatment of cancer refractory to conventional treatments alone. Clinical studies have recently shown that adding
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br Experimental section br Acknowledgements br Introduction
2024-04-01

Experimental section Acknowledgements Introduction DJ-1 is a highly conserved, homodimeric protein that was originally cloned as an oncogene capable of transforming K03861 in cooperation with activated ras[1]. DJ-1 is over-expressed in multiple tumor types and is positively correlated with
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Enhancers are short regions of DNA that are
2024-03-30

Enhancers are short regions of DNA that are bound by DNA-binding proteins (TFs) to increase the likelihood of a particular gene to be expressed. Importantly, enhancers can be identified, and classified, by their patterns of chromatin accessibility and of enrichment in certain histone modifications.
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In addition understanding the relationship
2024-03-30

In addition, understanding the relationship between human metabolic processes and dietary antioxidant intake would provide opportunities for altering the diet to improve health (Prior, 2015). Prior et al. (2007) emphasized that excess reactive oxygen species, which occurred during the metabolism of
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br Acknowledgements We thank the
2024-03-30

Acknowledgements We thank the National Natural Science Foundation of China (41576156), Shandong Province Science and Technology Development Plan (2015GSF121045), Yantai Science and Technology Development Plan (2015ZH078), and the Public Science and Technology Research Funds Projects of Ocean (No.
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It has been proposed that angiotensin
2024-03-30

It has been proposed that angiotensin II (Ang II) may upregulate COX-2 expression and the subsequent vasoconstrictor prostanoids production through the activation of AT-1 receptors in vascular smooth muscle cells (Hu et al., 2002). Additionally, this peptide is also able to stimulate the generation
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Recent studies revealed that certain plant derived compounds
2024-03-30

Recent studies revealed that certain plant-derived compounds can also interfere with AR function. One way of such an interference is by modulating its expression levels. This is the case for the two flavonoids quercetin and luteolin that have been reported to repress the function of AR by inhibiting
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SC 144 Earlier studies with SERMs identified that distinct
2024-03-30

Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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