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It is important to highlight that glucose dependent generati
2021-09-10
It is important to highlight that glucose-dependent generation of OMP of high magnitudes occurs due to the voltage-gating properties of VDACs, because only small magnitudes of OMP were obtained when the VDAC voltage sensitivity was zero (Fig. 5). These results indicate a possible physiological role
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Oltipraz has been shown to inhibit the growth of HCC
2021-09-10
Oltipraz has been shown to inhibit the growth of HCC Bisindolylmaleimide IV and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with
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Following nerve injury Shh expression is
2021-09-10
Following nerve injury, Shh expression is upregulated in neuronal cell bodies of the facial and sciatic nerves. Additionally, Shh appears to be required for normal regeneration in vivo, and promotes motor neuron survival in vitro (Martinez et al., 2015; Akazawa and Kohsaka, 2007). Based on these obs
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The absolute requirement for substrate prephosphorylation ra
2021-09-10
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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No compounds in this series showed any appreciable activity
2021-09-10
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in mal
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Oxidative stress results from the disequilibrium between lev
2021-09-10
Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Subsequently we decided to test whether the
2021-09-09
Subsequently, we decided to test whether the orexin pathway was involved (Delhanty et al, 2012, Delhanty et al, 2013, Pei et al, 2014). Orexin neuronal systems are known to control limbic and neocortical structures (Bonnavion, de Lecea, 2010, Sakurai, 2007). Orexin receptors and possibly orexin synt
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molar calculator The focused set of additional pyrazole
2021-09-09
The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro su
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br Acknowledgments br The study was funded by
2021-09-09
Acknowledgments The study was funded by the European Commission FP7-project Beta-JUDO (Grant 279153), and Swedish Diabetes Association (Grant DIA 2013-043) and Family Ernfors Foundation (Grant 150430). Free fatty 28170 receptors (FFARs) represent a family of G-protein coupled receptors (GPCR
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With the nitrogen containing heterocycle components and the
2021-09-09
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic Rufinamide (, and ), followed by deprotection by TFA, smoothly provided th
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Interestingly the subcellular localization of FBPase in hepa
2021-09-09
Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule thymidylate synthase inhibitor reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our
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One may ask whether induced loss
2021-09-09
One may ask whether induced loss, through chemical or genetic perturbation for example, of an essential cellular factor represents regulated cell death or simple loss of the homeostasis needed for life. For example, deletion of the Mdm2 gene, or inhibition of the MDM2 protein, results in cell death
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Recent efforts have also tried to identify cancer subsets
2021-09-09
Recent efforts have also tried to identify cancer subsets that are exquisitely responsive to EZH2i apart from those bearing EZH2 gene mutation (Knutson et al., 2012). The dysfunction of SWI-SNF complex, a chromatin-remodeling regulator that partially antagonizes the catalytic function of PRC2 comple
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br Introduction The airway epithelium is the first
2021-09-09
Introduction The airway epithelium is the first barrier against inhaled insults and the final barrier against internal forces (hydrostatic, inflammatory, and ischemic) that disrupt water and solute movement across the epithelium. This barrier is formed by adhesion of airway and alveolar epithelia
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Accordingly a bioassay guided approach was been used to stud
2021-09-09
Accordingly, a bioassay-guided approach was been used to study the bioactive compounds in VAS contribute to the α-glucosidase inhibitory and antioxidant activity. The 95% ethanol extraction of VAS was successively partitioned with petroleum ether, ethyl acetate and n-butanol. Ethyl acetate fraction
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