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br Acknowledgments This work was
2024-01-04

Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cul
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In the past few years several experimental findings
2024-01-04

In the past few years, several experimental findings have demonstrated a pivotal involvement of adenosine also in driving the phenotypic switch of macrophages. In particular, the stimulation of A2A and A2B receptors seems to play a critical role in switching macrophages from M1 to M2 phenotype [37,6
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br LO and the secretase complex Supporting this concept duri
2024-01-04

5LO and the γ-secretase complex Supporting this concept, during a recent trial testing the γ-secretase inhibitor semagacestat (LY 450139), AD patients actually experienced a functional decline compared to patients who took a placebo in addition to several other significant adverse effects (Doody
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Notably our preliminary results confirmed that fluoxetine
2024-01-04

Notably, our preliminary results confirmed that fluoxetine (SSRIs, 5–10 mg/kg) and duloxetine (SNRIs, 5–10 mg/kg) could not enhance memory function in the novel object recognition or step-down passive avoidance tasks (data not shown). In the present study, we also found that vilazodone showed had no
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From our in vivo studies and previously
2024-01-04

From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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CYP A is one of the key metabolizing
2024-01-04

CYP3A4 is one of the key metabolizing AZD6738 of the cytochrome P450 (CYP) superfamily of heme-containing monooxygenases. As the CYP family of enzymes plays important roles not only in the xenobiotic metabolism and detoxification of a large number of drugs, but also in the biosynthesis of endogenou
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Another topic for research will be the combination of other
2024-01-04

Another topic for research will be the combination of other cytotoxic agents with Aurora kinase inhibitors. Particularly interesting might be the combination of Aurora kinase inhibitors and agents that depend on the spindle checkpoint for their activity, such as the taxanes, given the importance of
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AP activation is known to upregulate downstream target
2024-01-03

AP-1 activation is known to upregulate downstream target genes including Ac-Endothelin-1 (16-21), human D1, c-myc, Bcl-xl, MMP-9, EGFR, and specific miRNAs that are involved in progression and metastasis of tumors. Moreover, matrix metalloproteinase-2 has been shown as a downstream gene of AP-1, tr
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Chlorogenic acid an abundant polyphenol
2024-01-03

Chlorogenic Arylquin 1 (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2) as compared wit
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Galanthamine HBr Introduction Hepatocellular carcinoma HCC i
2024-01-03

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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The proinflammatory cytokines and chemokines including
2024-01-03

The proinflammatory cytokines and chemokines, including IL-1β, TNF-α and MCP-1, mediate acute and chronic inflammation and play a role in the development of hypertension [2, [51], [52], [53]], cardiovascular diseases [4, 54] and renal injury [55, 56] in animal models and humans. Concerning the possi
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Due to metabolic variations it is important to consider argi
2024-01-03

Due to metabolic variations, it is important to consider arginine metabolism and dependency in specific contexts to identify precise patterns. This is best illustrated for ASS: while ASS deficiency correlates with worse prognosis in sarcomas, ASS levels positively correlate with a poor prognosis in
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T7 High Yield RNA Synthesis MD was the recipient of the Inte
2024-01-03

MD was the recipient of the Intergroupe Francophone de Cancérologie Thoracique (IFCT) Alain Depierre Grant in 2014. JP was the recipient of the ARISTOT (Association de Recherche, d’Information Scientifique et Thérapeutique en Oncologie Thoracique) grant in 2016. Conflicts of interest statement
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The lactam emerged as lead candidate due
2024-01-03

The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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In conclusion phenolic hydroxyl was introduced
2024-01-03

In conclusion, phenolic hydroxyl was introduced not only to C3 side chain but also to C6 or C7 position of the quinoxalinone core, resulting in a new group of ARIs candidates exhibiting antioxidant activity. Biological activity tests suggested that compounds were not only sufficient to inhibit ALR2
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