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We have previously shown that the antinociceptive effect of
2025-02-20
We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific Kenpaullone blockade or activation (Rojas-Corrales et al., 2000). Moreover,
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The present study showed for the first time that hirsutine
2025-02-20
The present study showed, for the first time, that hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, and isocorynoxeine in yokukansan can inhibit the 5-HT3 receptor current. These data indicate that part of the effect of yokukansan against the behavioral and psychological symp
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Introduction Adenosine monophosphate cAMP is a general purpo
2025-02-20
Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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br Funding br Introduction l
2025-02-20
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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The first rationally designed dual mPGES
2025-02-20
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic LY 2389575 hydrochloride - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives hav
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br Concluding remarks Autophagy ensures cell
2025-02-20
Concluding remarks Autophagy ensures cell homeostasis and survival through the continuous degradation/recycling of intracellular components. It can also represent a conserved, cell-intrinsic, defense mechanism against invading pathogens, including viruses. The autophagy process can be activated r
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R-848 The synthetic route for the aminobenzoxazole scaffold
2025-02-20
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 R-848 afforded compound . Aminobenzoxazole was formed by the reaction of compound with BrCN in EtOH. The solvent
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Zhang et al screened three thousand compounds library
2025-02-20
Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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Earlier studies showed that exposure of cells to IR
2025-02-20
Earlier studies showed that exposure of cells to IR caused ATM-dependent phosphorylation of 53BP1, as judged by electrophoretic mobility shift [24], [25], [26]. To date, the only known in vivo 53BP1 phosphorylation site(s) are Ser25 and possibly Ser29 [27]. In the course of our studies, we noticed t
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Methscopolamine br Conclusion br References and recommended
2025-02-19
Conclusion References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Nucleosome, the basic chromatin unit, is composed of DNA and core histones (H2A, H2B, H3 and H4) and organized into
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The current antifungal pipeline contains several categories
2025-02-19
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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br Introduction Increased renin angiotensin system RAS activ
2025-02-19
Introduction Increased renin-angiotensin system (RAS) activity and inflammation in cardiovascular-related regions of the central nervous system contribute to the overactivity of neurohumoral systems that promote volume retention, cardiac remodeling and serious cardiac arrhythmias in systolic hear
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Another class of AMPK regulator is
2025-02-19
Another class of AMPK regulator is peptidyl-prolyl cis/trans isomerase (PPIase) NIMA-interacting 1 (Pin1), which binds to a number of proteins and regulates oncogenesis and metabolic diseases (Khanal et al., 2013; Zhou and Lu, 2016). Pin1 has been shown to bind to and inhibit AMPK; therefore, at lea
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How do increased levels of ammonia as observed
2025-02-19
How do increased levels of ammonia as observed in clinical HE constrain synaptic plasticity? Numerous studies have investigated the modulation of signal transduction pathways activated in LTP or LTD irrespective of being necessary or sufficient for changes in synaptic efficacy (Wen et al., 2013). Ye
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When arachidonic acid is used as a substrate the
2025-02-19
When arachidonic cytoskeleton is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy derivative
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