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Replacement of the saturated propoxy group in compound with
2020-02-14
Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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Although the analysis described above goes far
2020-02-14
Although the analysis described above goes far to explain the mechanism of ciprofloxacin perturbations through CHK1 inhibition, it raises important questions about the mechanism by which WT RAS isoforms promote CHK1 S280 phosphorylation. Previous reports have shown that both the MAPK-RSK and PI3K-A
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In humans the ER is encoded by the gene
2020-02-14
In humans, the ERα is encoded by the gene ESR1, located on chromosome 6, locus 6q25.1 (Gosden, Middleton, & Rout, 1986). In addition to the full-length ERα isoform (66kDa), several shorter isoforms (36kDa, 46kDa) have been identified as a result of the presence of alternate start codons, or as prod
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In humans the ER is encoded by the gene
2020-02-14
In humans, the ERα is encoded by the gene ESR1, located on chromosome 6, locus 6q25.1 (Gosden, Middleton, & Rout, 1986). In addition to the full-length ERα isoform (66kDa), several shorter isoforms (36kDa, 46kDa) have been identified as a result of the presence of alternate start codons, or as produ
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During the past three decades platinum
2020-02-13
During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot
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This study had some limitations First
2020-02-13
This study had some limitations. First, a small number of HP patients were enrolled because of the extreme rarity of this disease, which may have caused some selection bias. Yokoseki et al., found no increase in Th2 cytokines, such as IL-4, in IHP patients (Yokoseki et al., 2014). The sensitivity of
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Similarly LTD concentration dependently enhanced AQP express
2020-02-13
Similarly, LTD4 concentration-dependently enhanced AQP4 expression in astrocytes (Fig. 3). The LTD4-enhanced AQP4 expression was not affected by pranlukast but inhibited by Bay u9773, a non-selective CysLT1/CysLT2 receptor antagonist [33]. Because no selective CysLT2 receptor antagonists are current
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br Next let s recall some definitions and notations from
2020-02-13
Next, let\'s recall some definitions and notations from [14] which are necessary to obtain the proof of Theorem 1. Let denote the CMV matrix whose Verblunsky coefficients replaced by , that is The corresponding extended CMV matrix is Recall the definition of in the proof of Theorem 2, replace
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To simulate the inhibition of the enzyme by
2020-02-13
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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Host cell invasion by tachyzoites
2020-02-13
Host cell invasion by tachyzoites relies on the secretion of numerous secretory proteins and plays a crucial role in maintaining infection [6]. ESA released by tachyzoites are highly immunogenic and induce either antibody-dependent or cell-mediated protective immunity [11], [44], [45]. To investigat
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Previous in vitro studies have demonstrated that DNA PK
2020-02-13
Previous in vitro studies have demonstrated that DNA-PK-deficient cell line (MO59J) is approximately 30-fold more sensitive to radiation than DNA-PK-proficient cell line (MO59K) [31]. Moreover, specific DNA-PK inhibitors SU11752 and wortmannin have been shown to sensitize GBM Blebbistatin (MO59K) t
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Multiple lines of evidence now indicate
2020-02-13
Multiple lines of evidence now indicate that mitochondrial decay is a fundamental factor that leads to alterations in energy metabolism in the aged heart (Hagen et al., 2002, Judge and Leeuwenburgh, 2007, Lesnefsky et al., 2001c). Nevertheless, the exact biochemical events that cause such an alterat
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It has been reported that CysLT receptors negatively regulat
2020-02-12
It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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br Materials and methods br Results br
2020-02-12
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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LGX818 Previous research has suggested that the acetylcholin
2020-02-12
Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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