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br Conflict of interest br Acknowledgments br Introduction
2024-07-06
Conflict of interest Acknowledgments Introduction Inflammation is a protective response of the microcirculation to harmful stimuli. Yet, excessive inflammation is potentially harmful and a characteristic of many chronic diseases [1]. 5-Lipoxygenase (5-LO, EC1.13.11.34) contributes to the in
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The inhibition of the exacerbated inflammatory
2024-07-06
The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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In this scenario the receptor tyrosine kinase inhibitors TKI
2024-07-06
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; P8-CPT-2Me-cA
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In conclusion we have designed and synthesized a
2024-07-06
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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The tumor suppressor function of LOX in
2024-07-06
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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Tumor suppressor ARF regulates the activity of p
2024-07-06
Tumor suppressor ARF regulates the activity of p53 by inhibiting the functions of Mdm2. ARF is induced by hyperproliferative signals emanating from oncogenic Ras, overexpressed c-myc, and from deregulated E2F . ARF prevents p53 degradation and leads to increased p53 function by sequestering Mdm2 to
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br Conclusions br Author declaration br Acknowledgements br
2024-07-06
Conclusions Author declaration Acknowledgements Introduction ASK1 scaffolding proteins ASK1 adaptor proteins Conclusions Scaffolding and adaptor proteins can coordinate the specific activation of a MAP3K-MAP2K-MAPK pathway in response to various stimuli. For example, both Desfor
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A different mechanism has been suggested for the role
2024-07-06
A different mechanism has been suggested for the role of TRX1 in ASK1 regulation based on disulfide bond-mediated ASK1 multimerization and its reduction through the thiol-reductase activity of TRX1 (Nadeau et al., 2007, Nadeau et al., 2009). In this model, oxidative stress induces intermolecular dis
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br Results br Discussion Although the value of ID
2024-07-06
Results Discussion Although the value of ID specialists in the USA has already been described in the literature, this study suggests that the same holds true for the Japanese healthcare environment [7], [17], [18], [19]. Valerio et al. reported that antifungal use in DDD decreased from 66.4 pe
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It remains to elucidate whether proteolytic activity is
2024-07-06
It remains to elucidate whether proteolytic activity is the cause or the consequence of changing levels of peptidergic substrates. In fact, in some cases, the expression of the enzyme does not necessarily parallel with its activity [26], [55], [57] and other factors such as a definite biochemical en
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br Concluding remarks Enhanced membrane
2024-07-05
Concluding remarks Enhanced membrane binding upon calcium stimulation in Hydroxy Bupropion suggests a pre-requisite step that involves a conformational change in LOX. This might facilitate it to tether to the membrane and regulate enzyme activity. The calcium binding loops and the putative activ
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However although in vitro studies in heterologous systems
2024-07-05
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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3-AP The potential use of derivatives belonging to this seri
2024-07-05
The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore
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Optimization of the B ring specifically
2024-07-05
Optimization of the B-ring specifically targeted preventing the oxidation of the ring system (). As described above, the 4-position of the phenyl ring provides the appropriate vector towards bulk solvent. - and -linked substitutions at the 4-position of the B-ring from the 4-fluoro-nitrophenyl inter
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Functional enhancers are often composed of binding motifs
2024-07-05
Functional enhancers are often composed of binding motifs of multiple key transcription factors to confer spatial and temporal regulation of genes in a certain context. In the uterus, the difference between the number of genes that have associated PGR occupancy and that of progesterone responsive ge
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