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ep4 Conventional aromatic radiofluorination via nucleophilic
2020-09-01
Conventional aromatic radiofluorination via nucleophilic substitution requires electron-withdrawing activating group(s) at the ortho or para position to achieve good radiolabeling yield. In the case of CJ-042794 (), the phenoxy substitution para to the fluoro group is considered an electro-donating
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Herein in continuation of our interest in designing new
2020-09-01
Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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OHC is a potent regulator of LXR mediated pathways
2020-08-31
25-OHC is a potent regulator of LXR-mediated pathways, that impact on pkc inhibitors lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OHC is able t
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Collectively our results indicate that GSK A functions as
2020-08-31
Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fig
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br Conclusion As far as we know this work constituted
2020-08-31
Conclusion As far as we know, this work constituted the first use of silver nitrate staining and sequential FISH in V. vinifera. This technique allowed the unequivocal identification of Ag-NORs and corresponding rDNA loci. Besides, silver nitrate staining and sequential FISH may bring new insight
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As for antiviral activity eight out of synthesized
2020-08-31
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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br Fragment based drug discovery FBDD
2020-08-31
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical nor-NOHA acetate space with libraries which are smaller in size, producing drug leads with high ligand-binding efficienc
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In humans individual differences in prefrontal
2020-08-31
In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia
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POE specialises Rogers definition of engineering
2020-08-29
POE specialises Rogers\' definition of engineering [37] to systems engineering as: As such, systems engineering becomes a problem solving exercise, the problem being, given a physical environment E, to find the system S that nebivolol hcl meets a real-world need N to the satisfaction of a group of
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Several reports have exploited the application of
2020-08-28
Several reports , , , , have exploited the application of HRM for detecting differentially methylated DNA. Even though DNA methylation analysis by HRM cannot determine the methylation status of individual CpGs, it does provide a robust and inexpensive method to differentiate DNA based on the overall
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The results showed that ethanol and acetaldehyde production
2020-08-28
The results showed that ethanol and acetaldehyde production was not affected by the presence of CPA-7. We observed that the concentration of ethanol increased throughout the assay up to 95–179 μL L-1 regardless of the treatment. The acetaldehyde concentration reached its highest values after 6–9 day
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br Introduction Cardiovascular disease continues
2020-08-28
Introduction Cardiovascular disease continues to be the leading cause of death in developed countries. Atherosclerosis, a chronic inflammatory cardiovascular disease, is characterized by the progressive buildup of oxidized low density lipoproteins in the arterial walls (Ross, 1999). In the develo
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As we all known hypoxia
2020-08-28
As we all known, hypoxia is a hallmark of tumour microenvironment, which is a key regulator of tumour growth and metastasis [4]. Hypoxia meditates a series of cellular responses including angiogenesis by activating transcriptional factor hypoxia inducible factor (HIF), which is consist of an obligat
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SPR was used to measure biomolecular kinetic interactions be
2020-08-28
SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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Based on the deduced amino acid sequence of the catalytic
2020-08-27
Based on the deduced amino Solithromycin sequence of the catalytic subunit of rG3DH, we could find sequence features that are highly conserved in FAD-harboring dehydrogenase, which include FAD binding motif and sequential cysteine residues in Cysteine-rich region. Several dehydrogenases share simil
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