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While we previously demonstrated that TraG is inhibited by s
2019-11-11
While we previously demonstrated that TraG is inhibited by specific transglycosylase inhibitors and that enzymatic activity is strongly reduced upon mutation of the potential catalytic core (Arends et al., 2013), the enzymatic mechanism of both domains was not assigned. Here, by mass spectrometry an
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br Introduction Addiction to opioids
2019-11-11
Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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In this context we initiated a program to
2019-11-11
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in Fruquintinib synthesis 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-dihydrotriazi
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The aberrant methylation of genes
2019-11-11
The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr
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br Results and discussion br Conclusion Novel and
2019-11-11
Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2019-11-11
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Cy7 maleimide (non-sulfonated) [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various
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We neither observed changes in midazolam eCLmet
2019-11-11
We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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Supported by the Austrian Science Fund FWF
2019-11-11
Supported by the Austrian Science Fund FWF (grant P22521-B18 to A.H.) and the Austrian National Bank (grant 14263 to A.H.). K.J. was funded by the PhD Program DK-MOLIN (FWF-W1241). Acknowledgements Introduction Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS), a more sev
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Elevated homocysteine has been considered to be
2019-11-11
Elevated homocysteine has been considered to be a risk factor for vascular dysfunction, vascular disease, and preeclampsia , . The methionine-homocysteine metabolism is responsible for supplying COMT with the methyl-group donor (-adenosyl methionine; SAM) necessary for 2-ME synthesis, and alteratio
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br Experimental br Results br Discussion In the
2019-11-11
Experimental Results Discussion In the last two decades, several studies have shown an important role for progestogens, and in particular ALLO, in the modulation of Schwann cell physiology, regulating several biochemical and functional parameters. The classical PR has been found both in rat
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br Materials and methods br Results br Discussion It
2019-11-11
Materials and methods Results Discussion It has been demonstrated that up-regulation of EPHB4 impaired trophoblast migration and invasion during placentation, which may contribute to the pathogenesis of preeclampsia [11], [24]. However, the upstream regulating mechanism of EPHB4 expression
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jasplakinolide Although information regarding the influence
2019-11-11
Although information regarding the influence of PGE2 on cardiac fibroblast cell growth is sparse, the effect of PGE2 on other cell types has been studied extensively, particularly in cancer and cancer cell lines where COX-2 is over-expressed. Constitutive high levels of COX-2 expression have been no
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To study the role of DNA PK in the response
2019-11-11
To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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At this stage it is still difficult to assign
2019-11-08
At this stage it is still difficult to assign specific domains to some of the regions observed in these structures, although some attempts have already been made (Brewerton et al., 2004). Clearly, higher resolution data is needed. In the future, even if an atomic structure of DNA-PKcs is determined,
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this research In general graphene nanoplatelets have many
2019-11-08
In general, graphene nanoplatelets have many useful features for the design of multifunctional composite materials, including excellent electrical and thermal conductivities, considerable weight-saving lightness, and high mechanical strength [26]. Moreover, they are characterized by a high specific
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