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Remarkably most of these molecules are also quite effective
2022-08-27
Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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To efficiently develop bioactive ligands even
2022-08-26
To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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Intracellular signaling pathways leading to IR
2022-08-26
Intracellular signaling pathways leading to IR injury are initiated by an increase in reactive oxygen species (ROS). This occurs principally at the time of initiation of reperfusion, which is accompanied by the re-admission of oxygen to the ischemic tissue. The resulting cascade of downstream events
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nisin Given the major differences between the molecular regu
2022-08-26
Given the major differences between the molecular regulation of the genes encoding HO-1 (HMOX1) in mice and humans, it is not appropriate to utilize mouse models for mechanistic analyses of human HMOX1[35]. In addition, it has been reported that drugs, such as statins, as well as stressors and the r
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GSTP c C T SNP
2022-08-26
GSTP1 c.341C > T SNP was genotyped in 90 patients tumor and 180 normal healthy individuals. The profile of GSTP1 c.341C > T CP-809101 hydrochloride mg and genotypes is shown in Table 2. The profile of the genotypes was in agreement with Hardy-Weinberg equilibrium (χ2 = 2.11). Minor allele frequency
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aldose reductase inhibitors Furthermore a direct thiol prote
2022-08-26
Furthermore, a direct thiol protective role of S-nitrosylation has been reported in animals [66]. Here, formation of higher order irreversible oxidative modifications, such as sulfinic and sulfonic acids were prevented by S-nitrosylation. All these observations underline the important role of ROS in
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br Positive regulation of gene expression
2022-08-26
Positive regulation of gene reverse transcriptase by Nrf2 Repression of Nrf2 by Keap1 Because many xenobiotic inducers of NQO1 and GST enzyme activities contain a thiol-reactive electrophilic moiety (i.e. are soft electrophiles), Paul Talalay and colleagues predicted in 1988 that they would b
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It appears that not all GPR agonists require a high
2022-08-26
It appears that not all GPR119 agonists require a high dose to elicit acceptable cyp450 inhibitors control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/
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mt t Our study has some limitations While
2022-08-26
Our study has some limitations. While our study provides data from a diverse multi-country setting, we did not have a sufficient sample size to investigate whether the relationship of micronutrients and mt t with CD4 recovery differed by country. We relied on measurement of deficiencies based on me
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In the brain hydrolysis of AG by
2022-08-26
In the brain, hydrolysis of 2-AG by MGL is the primary source of AA for conversion to PGs by cyclooxygenase (Nomura et al., 2011). PGE2 production is required for IL-1β-evoked synapse loss (Mishra et al., 2012). Here, we tested whether decreased PG levels contributed to the synapse protective effect
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br Evolution of multiple GnRH forms
2022-08-26
Evolution of multiple GnRH forms and GnRH receptors across vertebrates GnRH is an evolutionary ancient peptide that first appears prior to the protostome-deuterostome split, and is a member of the GnRH-adipokinetic hormone-corazonin superfamily of peptides (Roch et al., 2011, Roch et al., 2014).
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With taurine or other molecules
2022-08-26
With taurine, or other molecules that might be transported by Eaat2, an important area of research will be how such a chemical regulates sleep. Indeed, taurine has been described to act on the nervous system in disparate ways — it can act as an inhibitory neurotransmitter, but also has a well-charac
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Recently unimolecular multi functional peptides that combine
2022-08-25
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with PF-8380 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weight lo
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L-690,330 So in this study our results firstly demonstrated
2022-08-25
So in this L-690,330 study, our results firstly demonstrated that i.c.v. injection of ghrelin(1–7)-NH2 played a significant role in the modulation of the acute heat pain at the supraspinal level in mice. Our results showed that i.c.v. injection of ghrelin(1–7)-NH2 produced dose- and time- dependent
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One important discovery of our study is the identification
2022-08-25
One important discovery of our study is the identification of a pharmacological mechanism for the macrolide antibiotic erythromycin (EM) in promoting joint health. EM is a commonly used antibiotic that directly binds bacterial ribosomes to inhibit protein synthesis [66]. Although EM-like macrolide L
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