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QSAR based on the D structures of ligands plays an
2020-12-22
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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ecopipam br NADH and NADPH Turnover and the
2020-12-22
NADH and NADPH Turnover and the Putative Role of Alternative NAD(P)H Dehydrogenases Still very little is known about the metabolic function of external and internal alternative NADH:UQ oxidoreductases, and almost nothing is known about the mechanisms underlying their metabolic regulation, especia
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We then analyzed Ki proliferation index as
2020-12-22
We then analyzed Ki-67 proliferation index as a categorical variable by using 15%, essentially the median Ki-67 value in the entire study group (see above), to delineate low and high proliferation subgroups. By Fisher's exact test, both the type 1 versus non-type 1 EWS-FLI1 comparison (P = 0.047; Ta
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br Materials and methods br Results br Discussion
2020-12-22
Materials and methods Results Discussion The oestrogen agonist properties and androgen antagonist activities of parabens have been well documented by a variety of in vitro and in vivo assay systems over the past decade (Chen et al., 2007, Darbre and Harvey, 2008, Golden et al., 2005). To th
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ERR is expressed in several adult
2020-12-22
ERRγ is expressed in several adult and embryonic tissues but its biological role is still largely unknown [21]. Overexpression of ERRγ in breast cancer correlates with a favorable outcome [22]. In addition, ERRγ has been reported to inhibit the growth of prostate tumor MRS 2768 tetrasodium salt [23]
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br Acknowledgments br Significance The mechanisms underlying
2020-12-22
Acknowledgments Significance The mechanisms underlying the adverse effects of Epo-stimulating agents on the reduced survival of cancer patients are not well understood. Here, we identified EphB4 as an alternative Epo receptor, which triggers Src/Stat3 signaling via EphB4. We also showed that r
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br Iterative design approach overview
2020-12-22
Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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In principle in vitro techniques
2020-12-22
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized ryanodine lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombinant DNA
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Mouse Cyp a is a homologous
2020-12-22
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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We further assessed EBI expression in RRMS
2020-12-22
We further assessed EBI2 expression in RRMS patients before and during NTZ treatment. A significant increase of EBI2 expression was observed in memory CD4+ T cell subpopulations, but not in CD8+ T cell or in CD19+ B cell subsets of patients undergoing NTZ treatment, with a parallel gain in the migra
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br Authors contribution br Disclosure statement br Acknowled
2020-12-21
Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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br Acknowledgments br Introduction Cysteinyl leukotrienes Cy
2020-12-21
Acknowledgments Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic Papain Inhibitor australia and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, includ
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BW 723C86 hydrochloride We also evaluated the influence of t
2020-12-21
We also evaluated the influence of the number of CYP3A variant BW 723C86 hydrochloride (n=0 to 3) on the modifying effects on MDI and PDI. No clear allele dosage effect could be observed (data not shown). Discussion Prior reports for all four populations showed that an increase in prenatal Hg w
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Acknowledgements This work was supported
2020-12-21
Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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Moreover as shown in Fig f while the knockdown
2020-12-21
Moreover, as shown in Fig. 5f, while the knockdown of SMURF2 in wild-type G-15 has no significant effect on HSP27, in CK2α/α′(−/−) cells it leads to an increase of HSP27 level. These results suggest that SMURF2 affects HSP27 protein stability only when overexpressed, at least in our cell model. Th
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