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In conclusion the most salient observation from this study w
2022-01-21
In conclusion, the most salient observation from this study was that PAE reduced the expression of HDC protein expression in dentate gyrus, cerebral cortex, and cerebellum, but not in the caudate nucleus or ventral hypothalamus. The regional basis for this heightened sensitivity is not known, but it
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The only approved H R antagonist inverse agonist
2022-01-21
The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or
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ezh2 pathway Upon LPS stimulation ERK and STAT
2022-01-21
Upon LPS stimulation, ERK and STAT3 signaling pathways were activated in a time-dependent manner, and the phosphorylation of Y705 occurred later than that of S727 (Supplementary Fig. S5B). STAT3 is known to be phosphorylated on serine 727 (S727) by the mitogen-activated protein (MAP) kinase pathway
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For the SAR study human haspin kinase inhibitory
2022-01-21
For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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Acknowledgments br INTRODUCTION AND OBJECTIVES br METHODS br
2022-01-21
Acknowledgments INTRODUCTION AND OBJECTIVES METHODS RESULTS CONCLUSIONS Introduction Class 3 alcohol dehydrogenase (EC 1.1.1.1), also known as ADH5 chi polypeptide in humans, was first identified by Koivusalo et al. [1] as a NAD+-dependent hydroxymethylglutathione (HMGSH) oxidase. By
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In addition for the function
2022-01-21
In addition, for the function of GSNOR in brain, since GSNOR is the sole alcohol dehydrogenase isozyme in brain, the failure to detect ethanol dehydrogenase activity poses a problem if it is assumed that this enzyme has evolved and developed as a protective mechanism for ethanol detoxification in th
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GPR GPR GPR GPR and GPR
2022-01-20
GPR80, GPR81, GPR82, GPR93 and ψGPR79 all shared identities to P2Y GPCRs or P2Y-like oGPCRs. Previously, at least three different nucleotide receptor phenotypes have been observed in mammalian tissue, including GPCRs activated by AZ505 ditrifluoroacetate nucleotides (e.g. P2Y1 and P2Y11), uridine n
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Excessive extracellular glutamate can be removed from brain
2022-01-20
Excessive extracellular glutamate can be removed from Debio-1347 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 case of is
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Together our data are consistent with the idea that
2022-01-20
Together, our data are consistent with the idea that the antidepressant-like effect of a low dose of galanin administration in the DRN would be mediated by the activation of local GAL2. To support this hypothesis, we set an additional experiment to evaluate whether the antidepressant-like effect of
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However the clinical development of
2022-01-20
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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br PEPCK This enzyme decarboxylates and then
2022-01-20
PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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br Conclusions Symptoms from bilateral thalamic edema caused
2022-01-20
Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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Introduction Protein tyrosine phosphorylation plays key role
2022-01-20
Introduction Protein-tyrosine phosphorylation plays key roles in a variety of intracellular signaling pathways involved in cell proliferation, differentiation, gene expression, cell adhesion, and metabolic changes [1]. While receptor-type tyrosine kinases localize to the plasma membrane, most of no
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H R antagonism can prevent seizure development and improve
2022-01-20
H3R antagonism can prevent seizure development and improve working memory through the activation of histaminergic neurons (Huang et al., 2004, Zhang et al., 2003). In addition, we have recently found that H3R antagonism protects against ischemia-reperfusion injury via histamine-independent mechanism
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Rapalink-1 microRNAs miRNAs of approximately nucleotides
2022-01-20
microRNAs (miRNAs) of approximately 22 nucleotides play vital roles in cancer development and progression by regulating translational repression or decay of target messenger RNAs (mRNAs) through their binding to the 3′-untranslated regions (3′-UTRs) of target mRNAs with imprecise or precise compleme
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