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To identify structurally novel autophagy inhibitors a medium
2021-12-22

To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 qx 314 stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automated fl
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br Acknowledgements This work has been supported by TSTAR US
2021-12-22

Acknowledgements This work has been supported by TSTAR USDA and Florida Citrus Advanced Technology Program Grants to D.B., C.P and R.S. One of us (D.B.) is an established scientist fellow at the Oak Ridge Institute for Science and Education (ORISE). This research was supported in part by an appo
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Despite efforts over the past decade to shed light
2021-12-22

Despite efforts over the past decade to shed light on the endosomal maturation process and its underlying Rab conversion, the context in which all the involved protein components interact needs to be further elucidated. After defining single components and modules of the machinery important for endo
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ACET Ikaros utilizes chromatin remodeling to activate or rep
2021-12-22

Ikaros utilizes ACET remodeling to activate or repress the transcription of its target genes (Su et al., 2004). Ikaros directly associates with histone deacetylases HDAC1 and HDAC2 and can recruit them to the upstream regulatory elements of its target genes (Kim et al., 1999, Koipally et al., 1999a
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The synthesis of nitropyrimidine analogs
2021-12-22

The synthesis of 5-nitropyrimidine analogs – was outlined in . 4,6-Dichloro-5-nitropyrimidine, 4-methylsulfonylaniline and 2-fluoro-4-methylsulfonylaniline were prepared according to previously reported procedures., , Reaction of 4,6-dichloro-5-nitropyrimidine and substituted aniline in DMF yielded
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raf inhibitors Acknowledgements br Introduction The neurotra
2021-12-22

Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is
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Ironically another series of studies examining the role
2021-12-22

Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th
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Excessive extracellular glutamate can be removed from
2021-12-22

Excessive extracellular glutamate can be removed from arginase inhibitors interstitial fluids to the blood plasma for the maintenance of proper extracellular glutamate homeostasis in the mammalian central nervous system [[5], [6], [7]]. The glutamate concentration in the blood plasma increases in c
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Caffeine decreased EAAT and EAAT expression levels in
2021-12-22

Caffeine decreased EAAT1 and EAAT2 ABT263 levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resume, our data
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Importantly bioelectric circuits in tissues Fig A have a
2021-12-22

(4) Importantly, bioelectric circuits in tissues (Fig. 2A) have a capacity to store long-term patterning information. An example is planarian anterior-posterior patterning: during regeneration, each fragment cut from a worm needs to build a head and tail at their correct ends. This process is regula
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The first FPR ligand described
2021-12-22

The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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Corresponding to the different insulinotropic signaling the
2021-12-22

Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct ATI-2341 on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonists
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Interestingly the subcellular localization of FBPase in hepa
2021-12-22

Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule N-acetyl D-galactosamine sale 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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The current study identified the presence and location of
2021-12-21

The current study identified the presence and location of all four histamine receptors in the GI tract of 6 healthy adult dogs. Although no clinical signs of GI disease were noted, mild inflammation was noted in at least one section of the GI tract in all dogs based on WSAVA guidelines. Interpretat
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In our previous study we designed and synthesized
2021-12-21

In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic kl compound name (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro a
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