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Tacrine amino tetrahydroacridine I Fig was the first
2021-07-20
Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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As the primary model we selected LDL
2021-07-20
As the primary model we selected LDL-receptor knockout mice because these resemble the human plasma lipoprotein profile more closely. Currently, genetic models with reduced milk cholesterol content, which mimic cholesterol-free formula feeding, are unavailable. Thus, instead of modifying milk choles
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Several CHK inhibitors have been reported in the literature
2021-07-20
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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In the present study we determined concentration
2021-07-20
In the present study, we determined concentration–response relationships for selected synthetic progestogens using in vitro luciferase transactivation assays driven by PR, ARα and ARβ from Murray–Darling rainbowfish () and compared the profiles with those obtained from similar assays based on human
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br Results and discussion The effects of
2021-07-19
Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr
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UBA belongs to the non canonical E enzymes that
2021-07-19
UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5's adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral
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4-DAMP br Materials and methods br Results br
2021-07-19
Materials and methods Results Discussion ParI, the first C5-DNA-MTase from a psychrophilic bacterium to be characterized, displays DNA methylation activity in vivo and in vitro. Its biophysical characteristics are consistent with large regions of disorder including thermal unfolding transit
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Aspergillus nigerA niger is another filamentous fungus in wh
2021-07-19
Aspergillus nigerA. niger is another filamentous fungus, in which alternative dehydrogenases have been described. Filamentous fungi are a very important group of microorganisms that are used in industry (O’Donnell et al. 2011). Biotechnological production processes using these organisms are often hi
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As temperatures increase rates of spontaneous deamination al
2021-07-19
As temperatures increase, rates of spontaneous deamination also increase such that hyperthermophilic organisms must have efficient mechanisms for dealing with this potential hazard.8., 9. The hyperthermophile Methanococcus jannaschii has both a dCTP deaminase (encoded by the gene at locus MJ0430) an
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Altogether we have shown the presence of fully methylated DA
2021-07-19
Altogether we have shown the presence of fully methylated DAPK fragments in serum of ovarian cancer patients but also of women with uterine leiomyoma. This indicates the prerequisite for the analysis of not only healthy controls but also of women with other frequent non-cancer disease for the valida
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DAPK is a kD Ca
2021-07-19
DAPK is a 160-kD Ca2+/calmodulin (CaM)-regulated Ser/Thr kinase that mediates cell death. The activated forms of DAPK and DRP-1 are capable of inducing two distinct cytoplasmic events characteristic of programmed cell death, including membrane blebbing and the formation of autophagic vesicles (Inbal
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In S hexyl GSH non treated guinea pigs antigen
2021-07-19
In S-hexyl GSH non-treated guinea pigs, antigen-induced anaphylactic response was suppressed by montelukast, but not by BayCysLT2RA, indicating that this asthmatic response was basically CysLT1-receptor-dependent. On the other hand, the suppressive effect of montelukast was weakened by treatment wit
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Previous studies reported that combined administration of
2021-07-19
Previous studies reported that combined administration of licorice/GL and TWHF/TP showed reduced toxicity and equal or even potentiated therapeutic efficacy when treating arthritis (YS et al., 2006, YS et al., 2008, Zhang et al., 2007). Our findings that GL reduced exposure to TP in rats confirmed t
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A summary of the drug CDK hydrophobic
2021-07-19
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different compact the same value [77], which facilitates comparisons among different p
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Nuclear export mediated by CRM is initiated by an
2021-07-19
Nuclear export mediated by CRM1 is initiated by an interaction between RanGTP and the HEAT9 loop of CRM1, triggering a conformational change in the NES binding site that permits NES–cargo protein binding (Dong et al., 2009, Fung and Chook, 2014). Our docking simulation results predicted that DP2392-
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