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The synthetic route chosen for the preparation of the substr
2019-11-28
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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Creatinine Despite a high affinity for progesterone and
2019-11-28
Despite a high affinity for progesterone and a relatively high affinity for testosterone [7], the binding of progesterone and testosterone to CBG is often disregarded [1], [2], [3]. However, the concentrations of these two hormones varies considerably under both normal physiological and pathophysiol
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For statistical analysis the Statistical Package for Social
2019-11-28
For statistical analysis, the Statistical Package for Social Sciences (SPSS) was used (version 21.0; SPSSInc., Chicago, IL). Chi-square (x2) exact test was used for the comparison of categorical data, whereas Wilcoxon and Mann–Whitney U tests were used for the analysis of nonparametric variables bas
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The larger eukaryotic ligases such as LigI and
2019-11-28
The larger eukaryotic ligases, such as LigI and LigIV, also possess an additional N-terminal DNA-binding domain (DBD) that is required for efficient ligation (Fig. 1c) and enables these ligases to encircle DNA [17]. An equivalent helix–hairpin–helix domain is also present in the bacterial NAD-depend
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The Czech Republic is a country
2019-11-28
The Czech Republic is a country with increasing CDI incidence (1.1 cases per 10,000 patient bed-days in 2008–4.4 cases in 2011–2012 and 6.2 cases per 10,000 patient bed-days in 2012–2013) (Bauer et al., 2011, Davies et al., 2014) and relatively high rates of antibiotic resistant C. difficile strains
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Furan analogs and N methylpyrrole analogs had
2019-11-27
Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 dog is super cute affinity and an increased antagonist activity, while the corresponding chemical
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It has been reported that cAMP also
2019-11-27
It has been reported that cAMP also acts via Epac and Epac to attenuate CREB. However, in human monocytes ONO-AE1-329 (the EP4 receptor agonist used in this study) worked entirely through the cAMP-PKA pathway and not vis Epac [12]. Our data suggests that the cAMP-PKA-CREB pathway predominates for MU
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br Introduction Acylglycerol acyltransferases AGATs are pred
2019-11-27
Introduction Acylglycerol acyltransferases (AGATs) are predominantly responsible for triglyceride synthesis in the body, via two major pathways: the glycerol phosphate (GP) pathway (Kennedy, 1957) and the monoacylglycerol (MG) pathway (see Coleman and Lee, 2004, Yen et al., 2008). The final step
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br Results and discussion A systematic search for genes
2019-11-27
Results and discussion A systematic search for genes encoding H+-PPases was carried out by PCR using genomic DNA from a wide range of protozoa as templates and degenerate oligonucleotides, designed from amino ci-1033 domains conserved in H+-PPases of higher plants and the proteobacterium R. rubru
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ERRGO mice exhibited increased oxygen consumption decreased
2019-11-27
ERRGO mice exhibited increased oxygen consumption, decreased RER, high running endurance, and resistance to diet-induced weight gain. These changes are physiological hallmarks of increased aerobic capacity in mice and are a direct consequence of engineering highly oxidative and vascularized muscle b
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Cefpodoxime Proxetil As illustrated in Table monocyclic acid
2019-11-27
As illustrated in Table 3, monocyclic Cefpodoxime Proxetil analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9 exhibited
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In the context of E ligase drug discovery it
2019-11-27
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 res
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br Introduction br Structure of
2019-11-27
Introduction Structure of the Ku heterodimer associated to DNA The atomic structure of the Ku heterodimer, alone and bound to a small DNA fragment, was recently determined (Walker et al., 2001) and has significantly improved our understanding of DNA recognition by DNA-PK holoenzyme (Fig. 3). B
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Although the formation and toxicity of DPC
2019-11-27
Although the formation and toxicity of DPC is theoretically acceptable, it is difficult to evaluate the specific role of DPC and its repair enzyme MGMT in the cytotoxic and mutagenic effects because DPCs are estimated to constitute only 1%–3% of total DNA damage when abiraterone acetate mg are expo
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cisapride synthesis In these studies the inflammatory cytoki
2019-11-27
In these studies, the inflammatory cytokine IL-8 was demonstrated as one of the responsible molecules induced by CysLTs via activating CysLT2 receptors. IL-8 is synthesized in and released from mononuclear cells, macrophages, fibroblasts and airway epithelial cells, and it promotes inflammation as a
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