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The aniline R group was extensively explored
2019-07-19
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Experiments on the rat model of E coli pyelonephritis
2019-07-19
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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br Acknowledgments We thank Jon Clardy Juan Manuel Dom nguez
2019-07-18
Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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Contrary to genetic aberrations epigenetic methylation marke
2019-07-18
Contrary to genetic aberrations epigenetic methylation markers with broad coverage of OvCa subtypes were detected in primary tumors [21]. Ibanez de Caceres et al. [22] identified hypermethylation of BRCA1, APC, p16, p14, DAPK or RASSF1A in 50 of 50 primary tumors. Moreover the methylation pattern wa
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Significantly less is known about regulation of phytocystati
2019-07-18
Significantly less is known about regulation of phytocystatin gene expression. A genomic clone corresponding to the barley cystatin Icy gene has been characterized (Gaddour et al., 2001) and the function of its promoter region has been analysed by Martínez et al. (2005b). Bioinformatic analysis of t
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Cys LT have been shown to
2019-07-18
Cys-LT have been shown to be critical for stimulation of monocytes to produce various proinflammatory factors [32,67]. Fig. 3 shows results obtained with human peripheral monocyte-derived macrophages differentiated for 6 days with 20 ng/ml macrophage colony-stimulating factor (M-CSF) and challenged
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br Acknowledgments We thank the Lapaha Community and
2019-07-18
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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From materials science it is known that the
2019-07-18
From materials science, it is known that the differences in the annealing temperature is the main factor that mostly influences La (Takai et al., 2003, Cançado et al., 2006). In analogy, controlling the pyrolysis temperature and AG-1295 during residues burning might be a key aspect to reproduce the
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The second constraint indicates that
2019-07-18
The second constraint indicates that if the relationship between two components A and B is two-way, then there are at least two connectors, one with origin A and destination B, and another connector with origin B and destination A (OCL2 of Fig. 4). Therefore, at least one output port of the first co
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All of the studies referred
2019-07-18
All of the studies referred to above were on microvillous membrane from hSTB; however, there is little information regarding conductances in the basal membrane. Illsley and Sellers, using a fluorescent technique, determined the relative permeabilities of cations and chloride in basal membrane vesicl
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Resistance to avermectins has been associated with
2019-07-18
Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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The important role of miRNAs in cellular differentiation has
2019-07-18
The important role of miRNAs in cellular differentiation has been proposed recently. Previous studies had suggested roles for different miRNAs during osteogenesis [20]. Certain miRNAs could promote osteoblast differentiation, such as miR-194 [20], whereas others could inhibit the cell differentiatio
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In summary we have identified
2019-07-17
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was al
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Cathepsin S inhibitor where Next we evaluated whether DPP in
2019-07-17
Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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To assess whether the described cooperation between the EGFR
2019-07-17
To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope
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