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AD is an irreversible and progressive neurodegenerative dise
2021-10-18

AD is an irreversible and progressive neurodegenerative disease affecting the Protease Inhibitor Library which insidiously destroys memory, thinking skills and cognition. Originally described in 1906 by German physician Alois Alzheimer, AD is characterized by the presence of intraneuronal neurofibri
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br Visualizing single synaptic vesicle exocytosis
2021-10-16

Visualizing single synaptic vesicle Methscopolamine at CNS synapses We visualized the dynamics of individual synaptic vesicles as they fuse and immediately before fusion at the mammalian conventional synapses for the first time (Midorikawa and Sakaba, 2015). We use a calyx of Held terminal, a la
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When studying the potential of HATi for the treatment of
2021-10-16

When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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Fig summarizes the results for M concentration of the drugs
2021-10-16

Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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br Results br Discussion The present findings outline
2021-10-16

Results Discussion The present findings outline a novel regulatory mechanism for fasting-induced ketogenesis, which involves histamine release from mast SP2509 into the hepatic portal system, H1 receptor-mediated stimulation of liver OEA biosynthesis, and recruitment of the nuclear receptor PP
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The more important effect of pitolisant is related
2021-10-16

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced 5959 receptor release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenag
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The occurrence of naturally HCV NS resistance associated sub
2021-10-16

The occurrence of naturally HCV NS3 resistance-associated substitutions (RAS) affects virological outcome of DAA-based combination therapies [14], [15], [16], [17], [18], [19]. For the majority of NS3 protease inhibitors the frequency of natural occurrence of single RASs in HCV genotype 1-infected p
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br STAR Methods br Author
2021-10-16

STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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To test this concept we
2021-10-16

To test this concept, we took advantage of our large supply of various 2-pyridyl containing [3.1.0] cores (inactive with alkyl or aryl sulfonamides) and prepared the -methylimidazole sulfonamide analogs and (), as work form Merck demonstrated that the 2-pyridyl moiety was superior to the original
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SEN0014196 Hesperidin is an abundant and inexpensive plant f
2021-10-16

Hesperidin is an abundant and inexpensive plant flavonoid, largely derived from citrus species including sweet orange and lemon. Hesperetin (Hst) is the aglycone of hesperidin. Hesperidin and hesperetin have been reported to show a battery of pharmacological properties, including anti-hyperlipidemic
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br Glucose metabolism and diet Glucokinase
2021-10-16

Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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Olanzapine has been reported to attenuate
2021-10-16

Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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3'-O-(2-nitrobenzyl)-2'-dATP In summary two new flex
2021-10-15

In summary, two new flexible amine-functionalized quinolinium derivatives with far-red region emitting were prepared. The shorter-chain fatty amine side chain in the scaffold of was found to be a more promising G-quadruplex DNA fluorescent probe, suggesting the amine side group plays an important r
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Previous research has suggested that differences
2021-10-15

Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, la
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FGF signals can be transduced to the signaling cascades
2021-10-15

FGF signals can be transduced to the signaling cascades of RAS-MAPK or PI3K-AKT through FRS2 and GRB2, to the pathways of PKC or PKD via PLCγ and DAG, and to Ca2+-releasing cascade via PLCγ and IP3, finally affecting cellular proliferation, cellular survival, and angiogenesis [48]. By increasing syn
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