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Classical DHFR inhibitors such as methotrexate
2020-10-10

Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino teneligliptin residues as well as hydrophob
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Members of the Nudix family typically
2020-10-10

Members of the Nudix family typically contain a 23-amino-acid sequence (Nudix box) of GxExREUxEExGU, where U is usually Ile, Leu, or Val and x represents any amino acid. The EUxEE core residues serve as anchors for an Mg ligand that associates with a characteristic pyrophosphate linkage that is comm
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br Materials and methods br Results br Discussion In
2020-10-10

Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated 87 6 guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and LTD4[9],
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In conclusion high methylation levels of CDKL were observed
2020-10-10

In conclusion, high methylation levels of CDKL2 were observed both in HCC cell lines and tissues, which showed a negative association with mRNA expression. Moreover, treatment with demethylation agent in HCC cell lines could upregulate CDKL2 mRNA expression. The discovery of the epigenetic modificat
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br Transparency document br Acknowledgments This work was su
2020-10-10

Transparency document Acknowledgments This work was supported by the Ministry of Education, Youth and Sports of the Czech Republic (the National Program of Sustainability I, Grants LO1204 and LO1304), by the Czech Science Foundation (15-17282Y) and by Palacký University Olomouc (IGA_PrF_2017_0
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Recent data obtained with etifoxine suggest that facilitatio
2020-10-10

Recent data obtained with etifoxine suggest that facilitation of GABAergic inhibition may be also associated with an indirect mechanism implying activation of the peripheral benzodiazepine receptor with a subsequent increase in neurosteroid production (Schlichter et al., 2000, Verleye et al., 2005).
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In rats exposed to day of
2020-10-10

In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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br Conclusion br Introduction The morphological variability
2020-10-10

Conclusion Introduction The morphological variability of aquatic plants is well documented, and in some cases has seriously constrained taxonomic resolution (Sculthorpe, 1967, Santamaría, 2002). Many of these variations are caused by the extensive phenotypic plasticity of aquatic plants, but t
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ipi-145 receptor Synthetic peptides have proven highly valua
2020-10-10

Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of
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The phenolic hydroxyl group of ezetimibe
2020-10-10

The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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For the current studies we used the selective
2020-10-09

For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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EBI is known to play
2020-10-09

EBI2 is known to play a critical role in the induction of antibody responses in secondary lymphoid tissues.13, 14 However, little is known about the expression and function of EBI2 in human peripheral tissues. To our knowledge, this is the first report of increased EBI2 levels in peripheral tissues
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Western blotting and flow cytometry was employed to assess
2020-10-09

Western blotting and flow cytometry was employed to assess the DNA-PK inhibition of LTU28 and LTU31 in combination with radiation. It has been previously reported that phosphorylation of DNA-PKcs at the Thr2609 cluster plays an important role in DSB repair and resistance to radiation (Ding et al., 2
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Mutation in BRCT II domain W R either
2020-10-09

Mutation in BRCT-II domain (W893R) either in the full-length context or the C-terminal context greatly reduced the expression of LIG4 (Fig. 2B, Fig. 3B), suggesting the importance of BRCT-II domain in the maintenance of LIG4. In this regard, it might be noted that LIG4 protein was undetectable in Li
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br Limitations There are some limitations to take into
2020-10-08

Limitations There are some limitations to take into account when interpreting these results. Firstly, direct causation cannot be established in this cross-sectional study, and it may be the downstream effects of TNFα, such as increased fgf receptor inhibitor production, which are more proximally
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