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To investigate the mechanism of action of trisubstituted azo
2019-11-12
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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Estradiol the predominant circulating estrogen
2019-11-12
Estradiol, the predominant circulating estrogen in humans, it is mainly secreted by the granulosa cells of the ovarian follicles, and the corpora lutea, by the mechanisms indicated above. On the other hand, estretrol is synthesized exclusively during pregnancy by the fetal liver and reaches maternal
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br Experimental section br Acknowledgments
2019-11-12
Experimental section Acknowledgments This work was supported by the National Natural Science Foundation of China (NSFC, Grant No. 81573285 and No. 81602965), the Natural Science Basic Research Plan in Shaanxi Province of China (Program No. 2018JM7071 and No. 2017JQ8002), and the Fundamental Re
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To study systemic potential of the selected compounds as
2019-11-12
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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The elastase induced injury model has been
2019-11-12
The elastase-induced injury model has been shown to produce airspace enlargement, and increases in lung volume and compliance that are similar to those observed in human patients (Hantos et al., 2008, Hamakawa et al., 2011). Thus, this model, which has been used to study emphysema, should be adequat
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In this study we have explored a functional
2019-11-12
In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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Protein expression and purification A mL overnight culture o
2019-11-12
Protein expression and purification. A 3 mL overnight culture of E. coli BL21 (DE3) pLysS pGEX-6P-3-A1S_0222 was grown in Luria-Bertani (LB)-Medium (10 g/L tryptone, 5 g/L yeast extract, 5 g/L NaCl, pH 7.4, 100 μg/mL Amp) at 37 °C and 160 rpm. The overnight culture was diluted 1:100 into 200 mL LB (
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br Competing interests br Acknowledgements br Introduction D
2019-11-12
Competing interests Acknowledgements Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) in biomembranes to produce phosphatidic membrane transporter (PA) [1], [2], [3], [4], [5], [6]. To date, ten mammalian DGK isozymes (α, β, γ, δ, ε, ζ, η, θ, ι and κ) have been i
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The presence of H PPases in
2019-11-12
The presence of H+-PPases in parasitic protists raises the question of the physiological role of these proteins. So far, they had been extensively characterized mainly in higher plants, and some prokaryotes [1], [2], [3], [4], [5], [6], [7], [16], [20]. A common feature to all these organisms is tha
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itsa mg Within the Class II receptors the
2019-11-12
Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem itsa mg of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely related, as are D2 and
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The pyrrolo benzodiazepines PBDs are
2019-11-12
The pyrrolo[2,1-][1,4]benzodiazepines (PBDs) are a family of antitumour antibiotics that includes the natural products anthramycin and DC-81. They exert their cytotoxicity by covalently bonding to the exocyclic C2–NH group of guanine residues in the minor groove of DNA through their N10–C11 imine fu
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Cancer has been linked to
2019-11-12
Cancer has been linked to both genetic and epigenetic changes. Epigenetic modifications, mainly DNA methylation at CpG dinucleotides, affect the regulation of gene transcription without altering the gene\'s sequence. Short sequences rich in CpG dinucleotides (i.e., CpG islands) are often found in th
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br Conclusion In this review we have discussed how
2019-11-12
Conclusion In this review, we have discussed how inhibition of the CK2/CDK5 signaling axis protects WM only when inhibited before ischemia, while inhibition of the CK2/AKT/GSK3β signaling axis protects WM either before or after an ischemic injury in young, aging, and old WM (Fig. 3). CK2 activati
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Prenylation may turn a flavonoid from an agonist to an
2019-11-12
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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br Acknowledgments We thank the Lapaha Community and Nobles
2019-11-11
Acknowledgments We thank the Lapaha Community and Nobles (His Serene Highness Prince Kalaniuvalu Fotofili, Her Serene Highness Princess Marcella Taumoepeau Tupou Kalaniuvalu Fotofili and Her Royal Highness Mele Siu\'ilikutapu Kalaniuvalu Fotofili) and the Ministry of Internal Affairs (Government
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