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With the identification of small nonpolar substituents at
2021-10-18
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy
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The normal function of the FBPase enzyme is to
2021-10-16
The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa
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Despite such extensive analysis of Gcn homologs the
2021-10-16
Despite such extensive analysis of Gcn5 homologs, the function of C. albicans Gcn5 (CaGcn5) is not well understood. Therefore, in this study we investigated the role of CaGcn5 in filamentous growth, invasive growth and stress response of C. albicans. We also examined the subcellular distribution of
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Studies have demonstrated the paradoxical
2021-10-16
Studies have demonstrated the paradoxical role of HO-1 in tumorigenesis. At initial stages of carcinogenesis, it protects DNA by lowering the ROS-mediated mutational rate, but later, HO-1 promotes cancer cell survival and proliferation. One PDAC therapeutic strategy is to increase ROS production and
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Similarly towards the acylsulfamoyl benzoxaboroles
2021-10-16
Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chl
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Ras pathways are involved in the regulation of
2021-10-16
Ras pathways are involved in the regulation of virulence in Cryptococcus neoformans [7] and Candida albicans [8,9]. To verify the importance of Ras in the survival response of the fungus in the host, a pathogenicity test of P. brasiliensis was performed before and after treatment with the Ras inhibi
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Glycogen synthase kinase GSK a serine threonine kinase has b
2021-10-16
Glycogen synthase kinase-3 (GSK-3), a serine/threonine kinase, has been confirmed to be involved in some biological processes in NaCl or wound-treated plants (Chen et al., 2003, Hai et al., 2001, Jonak et al., 2000). NO has been recently recognized as a vital signaling compound in plants. The NO don
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tie2 It has been shown that GPR
2021-10-16
It has been shown that GPR55 receptors coupled to G12/13 proteins down-regulate reactive oxygen species (ROS) production and degranulation in human neutrophils [9]. MCs degranulation stimulated by IgE/Ag also requires the generation of ROS [64]; therefore, the possibility to explore the inhibitory a
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br Next we explored the SAR around the aryl
2021-10-16
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic MK 571 sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did not
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Methods br Results br Discussion The current study
2021-10-16
Methods Results Discussion The current study is the first to specifically investigate the role of hepatic GPR109A and GPR109B on HDL metabolism and response to niacin therapy. While niacin raises HDL-C levels in humans, it has been reported by others [20], [36] and confirmed by us here that n
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Considering that loss of LAG expression results in increased
2021-10-16
Considering that loss of LAG-3 Fluorouracil sale results in increased CD4+ T cell homeostatic expansion, and that the ability of a cell to proliferate is tightly coupled to its metabolic profile, we hypothesized that LAG-3 regulates naive CD4+ T cell metabolism. Our results indicate that, indeed, La
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Based on our finding that TFA modulates GlyR function
2021-10-16
Based on our finding that TFA modulates GlyR function and reports that TFA-bound RN 1734 can differ markedly from those synthesized without TFA, we retested a previously published dodecapeptide (D12-116) that also enhanced GlyR function but this time as a chloride salt (Tipps et al., 2010). No diff
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br Introduction Major depressive disorder MDD is a
2021-10-16
Introduction Major depressive disorder (MDD) is a disease with poorly recognized etiology. Currently used antidepressant drugs, which mainly affect synaptic neurotransmitter levels, show full clinical efficacy in only one third of patients (Rush, 2007). Thus it is now generally accepted that the
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br Experimental br Results br Discussion The use of Dex
2021-10-16
Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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In patients with type diabetes glucagon receptor antagonism
2021-10-16
In patients with type 2 diabetes glucagon receptor antagonism led lowered fasting glucose however not postprandial glucose levels [9], which may reflect that glucagon may not be of particular importance for the diabetic hyperglycemia upon a meal. Current glucagon receptor antagonists have however be
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