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Recent studies demonstrated that AHR has
2024-01-22
Recent studies demonstrated that AHR has an important role in the interplay between cancer metabolism and tumor-specific immunity. Tryptophan catabolism is increasingly recognized as a metabolic pathway that promotes tumorigenesis through its role in immune suppression [75]. The rate-limiting enzyme
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A selected set of these new derivatives was
2024-01-22
A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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Very recently Niessen et al have described the resensitizing
2024-01-22
Very recently, Niessen et al. have described the resensitizing effect of MB327 on nAChR performing solid-supported membrane (SSM)-based electrophysiological experiments (Niessen et al., 2016) using plasma membrane preparations obtained from Torpedo californica. These findings validated and underline
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In earlier experiments on snails a behavioral model was
2024-01-22
In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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Matthew et al synthesized and carried out SAR studies of
2024-01-22
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that Vicriviroc Malate 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (
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KPT-276 Phosphoinositide kinase PI K Akt has
2024-01-22
Phosphoinositide 3-kinase (PI3K)/Akt has been well demonstrated in the protection of myocardial cell against IR injury via increasing cardiomyocyte survival, inhibiting excessive autophagy, et al. (Kong et al., 2016). The KPT-276 of ERK1/2 also involves in the regulation of cardiac myocyte survival
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IGF signaling has been shown to induce chromatin changes via
2024-01-22
IGF-1 signaling has been shown to induce butein changes via interacting with MKK-p38 signaling (Serra et al., 2007) and by perturbing Foxo3a signaling (Stitt et al., 2004), among other mechanisms. The current study demonstrates that the acetyl group itself may be limiting, since IGF-1/ACL/acetyl-CoA
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br Experimental section br Abbreviations
2024-01-19
Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino 22(R)-hydroxy Cholesterol deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N
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Imatinib was first approved for the treatment of
2024-01-19
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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Here we have used transcriptome analysis of
2024-01-19
Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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The acetylcholinesterase AChE inhibitor tacrine THA exerts n
2024-01-19
The acetylcholinesterase (AChE) inhibitor, tacrine (THA), exerts neuroprotective effects in time- and does-dependent manners against glutamate neurotoxicity (Takada-Takatori et al., 2006a, 2006b) and amyloid-β protein toxicity in PC12, a pheochromocytoma line (Wang et al., 2002; Xiao et al., 2000).
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Over the past decade extensive research has been
2024-01-19
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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Phagosomes acquire some hydrolases early during
2024-01-19
Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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br Materials and method br Results br
2024-01-18
Materials and method Results Discussion Although several studies have showed the crude extracts of K. senegalensis possessed the anti-inflammatory and hypertensive activities (Olayinka et al., 1992). However, the anti-inflammatory effect and underlying molecular mechanisms of its bioactive
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br Conclusions br Acknowledgments br Introduction The surfac
2024-01-18
Conclusions Acknowledgments Introduction The surface water bodies are affected by effluents containing pollutants from wastewater treatment plants, storm water overflows and run-off from non-point sources like agricultural land and urban city surfaces. This relates to land-based sources occ
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