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br Results and discussion br Conclusion In summary a
2024-08-28
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic Phosphatase Inhibitor Cocktail 3 (100X in DMSO) group extending from the C-3 positi
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We wanted to investigate the influence of substituents
2024-08-28
We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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br Antioxidant polymers conjugates Natural
2024-08-28
Antioxidant-polymers conjugates Natural antioxidants are usually used as a substitute for synthetics but some degradation phenomena could influence their applications. For example, ascorbic Boceprevir as a natural antioxidant undergoes yellowish coloration as a result of oxidation [29]. Sing and
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br Acknowledgments br Introduction Angiotensin
2024-08-28
Acknowledgments Introduction Angiotensin II (AngII) is among the most potent vasoactive substances produced in humans. Its effects are numerous, from vasoconstriction to control of fluid and electrolytes balances. Many of the physiological and pathological effects of AngII are mediated by the
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Recent genome wide association studies have indicated SORL
2024-08-27
Recent genome-wide association studies have indicated SORL1 as a risk factor for AD (Meng et al., 2007, Rogaeva et al., 2007, Wen et al., 2013). SORL1, is expressed in neurons (Yin et al., 2015) and also regulates APP traffic from the cell membrane to the Golgi apparatus. A reduction in its expressi
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Since the publication of the guidelines data have
2024-08-27
Since the publication of the 2011 guidelines, data have continued to accumulate indicating that the cognitive decline in AD occurs continuously over a long period [6–8], and that progression of biomarker measures is also a continuous process that begins before symptoms [9–14]. Thus, the disease is n
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For patients who have taken advantage of the
2024-08-27
For patients who have taken advantage of the anti-TKIs and whose follow-up has been succeeded, some partial response has been noticed with 45% (9/20) for gefitinib, 39% (9/23) for erlotinib and 56.5% (13/23) for crizotinib. A disease progression has also been observed with 35% (7/20) for gefitinib,
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The enzyme mediated ATP sensing mechanism
2024-08-27
The enzyme-mediated ATP-sensing mechanism in zebrafish can be compared with previous studies in other animal species reporting that enzymatic conversion of chemicals in the peripheral olfactory organ results in either “activation” or “inactivation” of odorants and pheromones. In male silkmoth, the a
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It is worth mentioning that cordycepin as an
2024-08-27
It is worth mentioning that cordycepin, as an adenosine analogue, is structurally similar to adenosine. A previous study has shown that the anti-apoptotic effects of cordycepin are partially dependent on the activation of A1R [16], and cordycepin increases theta waves power density via nonspecific a
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Small RhoGTPases are single domain nucleotide dependent bina
2024-08-27
Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine
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br Conclusion br Conflicts of
2024-08-27
Conclusion Conflicts of Interest/Disclosures Acknowledgement This study was funded by the Ministry of Science of the Republic of Serbia (grant #175083). Introduction Myasthenia gravis (MG) is an antibody-mediated, neuromuscular transmission disorder, where the targets are postsynaptic p
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Although experiments on animals and cells
2024-08-27
Although experiments on animals and cells indicate that antioxidant and free radical scavenging agents have protective effects against brain damage, the results of preclinical trials are not as encouraging. Edaravone is a type of free radical scavenging drug that was first used as a neuroprotective
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In conclusion we have designed and synthesized a
2024-08-27
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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Aurora A or B selective and
2024-08-27
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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There are in contrast many studies demonstrating that sex st
2024-08-27
There are in contrast many studies demonstrating that sex steroids modulate 3'-O-(2-nitrobenzyl)-2'-dATP synthesis processing of stimuli related to reproduction and this correlates with the observation that steroid receptors and aromatase are expressed in many brain nuclei that are part of the olfa
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