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Here we report discovery of highly selective pan Aurora
2023-02-06

Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of nitric oxide synthase inhibitor bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of t
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br Conclusion In summary screening
2023-02-06

Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b
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Aromatization of the pyrrole ring
2023-02-06

Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Apoptosis signal regulating kinase ASK
2023-02-06

Apoptosis signal-regulating kinase 1 (ASK1, also referred to as MAP3K5)(Ichijo et al., 1997) participates in many different stress responses, including apoptosis (Chang et al., 1998, Chen et al., 1999, Ichijo et al., 1997, Kanamoto et al., 2000, Noguchi et al., 2008, Saitoh et al., 1998, Tobiume et
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br Discussion Arginase and Arginase are homologous
2023-02-06

Discussion Arginase 1 and Arginase 2 are homologous enzymes that consume l-arginine to produce l-ornithine and urea [14], [15]. These enzymes compete with NO synthases for the same substrate [14], [15], [30], and therefore may reduce NO production [21], [24], [30]. The colocalization of arginases
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Previously we have detected the expression of APJ
2023-02-06

Previously, we have detected the expression of APJ receptor on stomach projecting QS 11 in DMV, in addition, icv administration of apelin-13 induced a remarkable c-Fos activation in those cells which were previously marked by a retrograde neuronal tracer fast blue (Birsen et al., 2016). Moreover, w
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br Acknowledgement br Introduction Estrogens play an
2023-02-06

Acknowledgement Introduction Estrogens play an important role in the development and progression of breast cancer (McGuire et al., 1976; Clemons and Goss, 2001). 17β-Estradiol (E2), the most biologically active estrogen in breast tissue, functions via its nuclear receptors, estrogen receptor (
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The first and the best characterized mechanism of
2023-02-06

The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic CGS 35066 receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional molecules suc
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About this report Alzheimer s Disease Facts and Figures
2023-02-06

About this report 2018 Alzheimer's Disease Facts and Figures is a statistical resource for U.S. data related to Alzheimer's disease, the most common cause of dementia. Background and context for interpreting the data are contained in the Overview. Additional sections address prevalence, mortality a
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A disfun o cognitiva p s operat ria
2023-02-06

A disfunção cognitiva pós‐operatória é uma síndrome perioperatória bem reconhecida, consequência da anestesia e cirurgia cuja causa exata permanece por esclarecer. De que forma Chlorprothixene disfunção cognitiva pós‐operatória e a doença de Alzheimer podem estar ligadas permanece uma questão em est
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To this the evidence of opposite effects of noradrenaline an
2023-02-06

To this, the evidence of opposite effects of noradrenaline and adrenaline on the striatal firing initiation (Fig. 6, Fig. 7) should not be ignored, because the striatum is related to controlling action timing by regulating the firing increase rate (Tanaka and Kunimatsu, 2011). Although the ligand su
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Previous work established interactions between
2023-02-06

Previous work established interactions between CRF and KOR systems in regulating attention (39). The CRF antagonist ANT attenuated, but did not completely reverse, the effects of PACAP (.5 µg) and did not have any effects on its own (Table 2). There were no significant differences in performance amo
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br Conclusions and clinical relevance Astrogliosis and an
2023-02-06

Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic tandospirone is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK i
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If overexpression of ADK is
2023-02-06

If overexpression of ADK is sufficient to induce spontaneous seizures, then reduction of ADK in engineered mice should prevent epileptogenesis. The generation of mice with moderately reduced levels of ADK in brain rather than complete ADK deficiency seems to be essential, since several lines of evid
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Chromatin proteins play important roles in
2023-02-01

Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian Neuregulin/Heregulin-1β (NRG-1β/HRG-1β), human recombinant protein is transcr
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