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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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Because most fusion detection methods were developed
2019-11-11
Because most fusion detection methods were developed to analyze paired-end reads (and especially Illumina data), they are not suitable for identifying fusion junction-spanning reads in single-end Ion Torrent libraries. Therefore, we developed the FusionDetect algorithm (implemented in the ChildDecod
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In bone PGE exerts both anabolic and catabolic
2019-11-11
In bone, PGE2 exerts both anabolic and catabolic effects [6], [7], [8], [9]. Administration of PGE2 to mice lacking each of the four prostanoid receptors identified EP4 as the primary mediator of PGE2-induced bone formation [10]. While the role of EP1 in osteoblastic differentiation and bone metabol
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The in vitro enantioselective metabolism
2019-11-11
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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