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The data from drug screening in P berghei Fig D
2020-09-24

The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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In this context we initiated a program to develop new
2020-09-24

In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in AZD1080 replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structura
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Nitric oxide NO is synthesized by
2020-09-24

Nitric oxide (NO) is synthesized by conversion of the l-arginine to NO and l-citrulline through reaction which is catalyzed by nitric oxide synthetase (NOS) (Knowles and Moncada, 1994). NO as an important molecule not only play a role as second messenger but also binds to cytochrome c oxidase and de
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A cocktail approach can detect the
2020-09-24

A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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br Materials and methods br Results
2020-09-24

Materials and methods Results The monoclonal antibody (mAb), 12G5, reacts specifically with the human fusin protein and recognizes the protein on many T-cell lines such as the SUP-T1 thymidylate synthase inhibitors (Endres et al., 1996). As shown in Fig. 1, AMD3100 at 25 μg/ml completely inhib
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jnk inhibitor The anxiolytic like responses produced by anti
2020-09-24

The anxiolytic-like responses produced by anti-SVG-30 suggests that CRF2 receptors mediate not only the elicitation of anxiety behavior induced by prior stress, i.e. conditioned freezing, but also unconditioned anxiety behavior induced by exposure to the unfamiliar environment of the elevated plus m
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In a previous study we reported that
2020-09-24

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in gap junction reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to inve
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br Methodology The following subsections describe the steps
2020-09-24

Methodology The following subsections describe the steps of the Systematic Literature Review (SLR) process we followed [9]. Results In our review of the literature, we used the definitions provided by the IEEE Standard Computer Dictionary [15] to categorize the claims about the effectiveness
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A comparison between tinnitus and
2020-09-24

A comparison between tinnitus and controls subjects showed increased activity in the left AUD and PHC for the gamma frequency band. The link between gamma band activity in the AUD and tinnitus has been identified using both EEG (van der Loo et al., 2009) and MEG (Weisz et al., 2005, 2007). This is s
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The need for dedicated DAPT updates is well justified by
2020-09-24

The need for dedicated DAPT updates is well justified by the large amount of data and new information generated in the field over the past few years. As expected, the ACC/AHA and ESC updates contain large areas of overlap as well as some differences. Differences were largely explained by the differe
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br Experiments br Numerical simulations br Discussion br Con
2020-09-23

Experiments Numerical simulations Discussion Conclusions By large-caliber PELE with various d/D against RHA plate at low velocity of 415 m s−1, impact experiments against 30 mm RHA target were carried out. Numerical simulations were also conducted to monitor progress of PELE expansion an
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Enzyme activity loss during the hydrolysis process has tradi
2020-09-23

Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important
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bcrp inhibitor br Halogenases Enzymatic C H activation leadi
2020-09-23

Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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br Material and methods br Results
2020-09-23

Material and methods Results Discussion The results show for the first time that DDRs may be involved in the pathogenic mechanisms of neurodegenerative diseases. We found that DDR1 and DDR2 levels are up-regulated in post-mortem AD and PD brains, suggesting that these receptors play a role
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High concentrations of kC may also arise from
2020-09-23

High concentrations of 7kC may also arise from dietary intake of processed cholesterol-rich food, likely favoring or worsening inflammatory bowel disease (IBD) [5,13]. Furthermore, IBD has been associated with a dysregulation of colonic 11β-HSD expression, exhibiting increased 11β-HSD1 and decreased
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