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Nicastrin is heavily glycosylated contributing KDa to the
2021-09-17
Nicastrin is heavily glycosylated, contributing 40–70KDa to the molecular weight of human γ-secretase. Among the 16 predicted N-linked glycosylation sites in the ECD, 11 have been unambiguously identified. The glycans appear to mostly stabilize the local structure, thus contributing to the folding a
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nf-κb pathway br Acknowledgements This work was supported by
2021-09-17
Acknowledgements This work was supported by grants of the Argentine National Research Council (CONICET, PIP 0662). The authors express their appreciation to the Transmission Electron Microscopy Service (MET) of the Faculty of Veterinary Medicine of the National University of La Plata (Argentina)
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Also a large number of small molecules
2021-09-17
Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [
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This SAR work led to the identification of compound
2021-09-17
This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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DZNep is a PRC inhibitor that
2021-09-17
DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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Our observation that glioblastoma tumor cells
2021-09-17
Our observation that glioblastoma tumor cells express ETA-R in 6/10 cases contrasts with a recent publication reporting ETB-R expression in these tumors [17]. The reason for the discrepancy between that report and the present study might be due to the fact that glioblastomas with oligodendroglial co
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br Retrieval requires histamine H receptors
2021-09-16
Retrieval requires histamine H1 receptors in dorsal hippocampus Retrieval is a dynamic process that requires neurotransmitter regulation (Barros et al., 2000, Barros et al., 2001). Recently, histamine, and histaminergic transmission has entered the list of putative neurotransmitter modulators of
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Studies have demonstrated the paradoxical
2021-09-16
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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The molecular mechanisms underlying spindle orientation are
2021-09-16
The molecular mechanisms underlying spindle orientation are still largely unknown. Budding yeast has been used to study spindle positioning and asymmetric cell division. Indeed, after cytokinesis, daughter cells have different sizes. The cell division plane is established early in the cell cycle and
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During pain signal transmission glutamate is released into t
2021-09-16
During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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br Results br Discussion Arc p forms a ternary complex
2021-09-16
Results Discussion Arc1p forms a ternary complex with ScMetRS and ScGluRS and acts as a tIF in trans of both synthetases to improve their catalytic efficiencies.20., 24. The human homolog of Arc1p, the p43 protein, is associated within a multi-enzyme complex containing nine aminoacyl-tRNA synt
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Compound was obtained as a yellow crystal acetone
2021-09-16
Compound was obtained as a yellow crystal (acetone). And the molecular formula of was established as CHO on the basis of a quasi-molecular ion at / 331.0799 [M+H] (calcd. for 331.0818) in its HR-ESI-MS. Compound showed H and C NMR similar to those of AZ 628 . However, The H NMR spectrum of contained
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Three main transport systems are involved in solute loss
2021-09-15
Three main transport systems are involved in solute loss and red cell dehydration (summarised in Fig. 1: Lew and Bookchin, 2005): the deoxygenation-induced cation conductance (sometimes termed Psickle), the Ca-activated K+ channel (or Gardos channel) and the KCl cotransporter (KCC). Psickle is activ
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The observed CORT induced increase in Cx phosphorylation at
2021-09-15
The observed CORT-induced increase in Cx43 phosphorylation at S368 may also contribute to GJIC disruption. Gap junction channel permeability is modulated through connexin phosphorylation (Moreno and Lau, 2007). Specifically, the phosphorylation of Cx43 on S368 has been previously shown to decrease i
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In a follow up study the same research
2021-09-15
In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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