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The nuclear receptor NR superfamily
2019-11-18
The nuclear receptor (NR) superfamily of ligand regulated transcription factors has proven to be a rich source of targets for the development of therapeutics for a wide range of human diseases. The NR3B subfamily known as the estrogen-related receptor (ERRα[NR3B1], ERRβ[NR3B2] and ERRγ[NR3B3]) regul
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As proof of principle the effect of
2019-11-18
As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration
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Recent studies from the literature
2019-11-18
Recent studies from the literature have identified new Riociguat of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-tolylurea (16d),
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Thalidomide Although enantioselective accumulation of metala
2019-11-16
Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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br Conclusions This study showed that in EOC cells
2019-11-16
Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC jw 2 with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed at the promoter of thi
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br Chemistry The test compounds listed in Table Table
2019-11-16
Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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During host cell interactions G intestinalis trophozoites
2019-11-16
During host-cell interactions, G. intestinalis trophozoites up-regulate several cell-associated proteins, including high-cysteine membrane proteins (HCMPs) and variant surface proteins (VSPs) [8]. The parasite also releases around 200 proteins upon host-cell contact, including many proteases [9,10].
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CDK lacks DNA binding domains
2019-11-16
CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PAX
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Two major mechanisms including apoptosis and oxidative stres
2019-11-16
Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,
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LVDP values of at the
2019-11-16
LVDP values of ~80% at the end of reperfusion. L-NAME treatment did not modify the contractility detected in ischemic control hearts but annulled the actions of BZ acquiring LVDP values up to 40% (Fig. 4 A). A similar pattern was observed when +dP/dtmax was analysed (Fig. 4 B). LVEDP, as an index o
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In conclusion we have shown that
2019-11-15
In conclusion, we have shown that the cellular effects produced by SFN in NSCLC BRD4770 are largely mediated by SFN-induced production of ROS. Cells with higher levels of EGFR were more resistant to SFN treatment and showed resistance to SFN-induced apoptosis, suggesting that high EGFR levels prote
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We found that both DDR and DDR ECD
2019-11-15
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a rec
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Converging evidence suggests that reduced glutamate transmis
2019-11-15
Converging evidence suggests that reduced glutamate transmission in the LS is linked to increased anxiety-like behaviors (Radulovic et al., 1999, Henry et al., 2006, Bakshi et al., 2002, Liu et al., 2004). Therefore, attenuated CRF1 receptor-mediated excitatory transmission in the LS following ASV-
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Here we report that ILC
2019-11-15
Here, we report that ILC3s sensed oxysterols through GPR183, which was highly expressed by LTi-like ILC3s. 7α,25-OHC-synthesizing enzymes were produced by fibroblastic stromal rq 1 found in intestinal lymphoid structures, and the GPR183 ligand 7α,25-OHC acted as a chemoattractant for ILC3s. GPR183
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Our previous studies indicate that EBI
2019-11-15
Our previous studies indicate that EBI2 is involved in the regulation of pro-inflammatory responses and inter-cellular communication under pathophysiological conditions such as LPS challenge (Rutkowska et al., 2016b). The data showed that media taken from LPS stimulated astrocytes induces macrophage
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