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The take home message here is
2024-12-18
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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Zhang et al screened three thousand
2024-12-18
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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Ryoichi et al modified potent
2024-12-18
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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The amino hydroxy methyl isoxazolepropionic
2024-12-18
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic Ipratropium Bromide (AMPA) receptor is also enriched in postsynaptic striatal neurons (Bernard et al., 1997, Kondo et al., 2000, Reimers et al., 2011). Its activity is subjected to the regulation by a mechanism involving phosphorylation (Lu and Ro
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The protective role of HMW
2024-12-18
The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid
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There is a delicate balance between ROS generation and scave
2024-12-18
There is a delicate balance between ROS generation and scavenging by the protective antioxidant defenses in the cell. Antioxidant systems present in the tandospirone include enzymes like superoxide dismutase (SOD), catalases, glutathione peroxidases (GPxs) and peroxiredoxins (PRxs) (Fig. 3) [38]. SO
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Of the infants in the study there
2024-12-17
Of the 580 infants in the study, there were 106 twin deliveries and 10 triplet deliveries. There was no difference in prenatal antibiotic exposure between multiple and singleton births. Nevertheless, analysis of maternal antibiotic use was based on the 309 individual mothers who were provided Pancur
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In summary the CV and renal benefits of sacubitril valsartan
2024-12-17
In summary, the CV and renal benefits of sacubitril/valsartan in HF patients are attributed to the increased levels of peptides that are degraded by neprilysin and the simultaneous inhibition of the effects of AT1 receptor by valsartan (Fig. 1). Physical and chemical properties Sacubitril/Valsar
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br Conflict of interest statement br Introduction Tanshinone
2024-12-17
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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We found that decreased Ng levels lead to a lower
2024-12-17
We found that decreased Ng levels lead to a lower threshold for LTD induction at L4–L2/3 synapses. Previous studies in hippocampal slice culture have shown that LTD at individual synapses induces spine elimination at both the targeted synapse and selective neighboring synapses when spines are monito
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br Conclusion These studies broadly demonstrate that dopamin
2024-12-17
Conclusion These studies broadly demonstrate that dopamine and endocannabinoid signaling in the NAc can have diverse effects on AMPAR-mediated synaptic function depending on previous psychostimulant experience. Here, we examined mechanisms underlying the depotentiation of AMPAR-mediated synaptic
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Similarly compound was prepared from aldehyde d by
2024-12-17
Similarly, cid calculator 13 was prepared from aldehyde 8d by following similar procedures (Scheme 3). Condensation of 13 with 7b or 7e provided the corresponding amides 9j or 9k, which then went through O-debenzylation by BCl3 to deliver the final compounds 10j and 10k in 37% and 32% overall yield
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br Adiponectin receptors in colorectal cancer development
2024-12-17
Adiponectin receptors in colorectal cancer development APN receptors expressed in CRC tissue may mediate its effects on cell expansion and cell death (Byeon et al., 2010). It was observed that the expression of AdipoR1 and 2 is higher in CRC tissue than in counterpart healthy tissues (Williams et
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Adenosine A A agonists have been shown to
2024-12-17
Adenosine A2A agonists have been shown to significantly reduce albuminuria in diabetic mice as well as plasma creatinine [24]. Proteinuria was greater in diabetic A2A knock-out (KO) mice than diabetic wild type (WT) mice [24]. Consistent with these findings, our laboratory initially found that prote
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Adenosine is a ubiquitous homeostatic purine nucleoside that
2024-12-17
Adenosine is a ubiquitous homeostatic purine nucleoside that accumulates extracellularly in response to metabolic stresses such as hypoxia and inflammation. Activation of either G protein-coupled adenosine receptors (ARs; A1R, A2AR, A2BR, and A3R) by extracellular adenosine can modulate cell signali
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