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Second the phosphorylation events e g Thr
2024-05-22
Second, the phosphorylation events (e.g., α-Thr172 and β-Ser108) needed for AMPK activation by small molecules binding at the ADaM or other sites remains unclear. Within the β-GBD, phosphorylation of β1-Ser108 was shown to be required for the activation by small molecules binding in the ADaM site, s
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br Materials and methods br Results br Discussion Endophilin
2024-05-22
Materials and methods Results Discussion Endophilin A1 is a membrane-binding protein that is mainly distributed in the central nervous system (Giachino et al., 1997), localizes in the dendritic shafts and spines of mature neurons (Yang et al., 2015), and relates to the function and morpholo
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Analysis of the enzyme activity expressed as rate
2024-05-22
Analysis of the enzyme activity, expressed as rate of product formation per unit serum volume (20μl), between the diagnostic groups revealed that ApB activity was significantly decreased in the patient group both at recruitment and after 13months when the substrate concentration used was 1.5mM (pH-L
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There are human genes in the
2024-05-22
There are 12 human genes in the SLC5A family, and 6 of these are expressed in human heart (Table 2). Little is known about SGLT proteins in the heart. Zhou et al. [56] reported the presence of SGLT1 mRNA in the human heart. Researchers have found that levels of SGLT1 mRNA in heart are approximately
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E3330 sale The inflammatory cytokine IL is an additional fac
2024-05-22
The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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Further evidence for action mechanism was provided
2024-05-22
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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br Experimental procedure br Introduction Migraine is
2024-05-22
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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br Adenosine as a mediator of procedures used to manage
2024-05-22
Adenosine as a mediator of procedures used to manage pain The issue of caffeine Caffeine, from dietary sources, is perhaps the most widely consumed behaviorally active agent in the world (Fredholm et al., 1999). Initial characterization indicated caffeine had a higher affinity at A1−, A2A− and
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br Conflicts of interest br Acknowledgments The authors ackn
2024-05-21
Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic Eng
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pde inhibitors br Results and discussion br Conclusion A ser
2024-05-21
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen pde inhibitors
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Exposure to cisplatin with ATR inhibitor
2024-05-21
Exposure to cisplatin with ATR inhibitor resulted in an increase in cisplatin-DNA adducts, especially in cells with ATM deficiency. This finding indicates that suppressing ATR-Chk1 signaling with VE-822 enhances cisplatin activity by enabling the drug to form DNA adducts. Therefore, VE-822 may incre
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From an historical perspective ligands for GPCRs
2024-05-21
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Fmoc-Gly-OH synthesis or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous l
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It has been proposed that a
2024-05-21
It has been proposed that a PrP pathogenic mechanism is a toxic gain of function secondary to the misfolding of mutated PrP. However, such a mechanism might not apply to all mutant PrP species, since some mutations had little effect on the stability and folding kinetics of PrP (Swietnicki et al., 19
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It has been well established that shortly after systemic inf
2024-05-21
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the Diosmetin sale and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADPH o
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br AR signaling and urothelial cancer progression As
2024-05-21
AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et
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