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To develop antagonists selective for the mouse EP receptor w
2019-11-27
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic azd9291 () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde . 4
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(-)-epicatechin receptor PET CT static images of F
2019-11-27
PET/CT static images of F-CJ-042794 acquired at 1h p.i. from LNCaP tumour-bearing mice with/without co-injection of non-radioactive CJ-042794 (50μg) are shown in . The LNCaP tumours were clearly visualized in PET images with a moderate tumour-to-background contrast. High radioactivity accumulation w
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As retinol was not inducing any
2019-11-27
As retinol was not inducing any of the isoforms of CYP450 responsible for the bioactivation of paracetamol, we decided to examine retinol\'s effect on renal and hepatic glutathione to determine whether retinol was potentiating hepatotoxicity through a mechanism of glutathione depletion. Studies, uti
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br Acknowledgments This work was supported by
2019-11-27
Acknowledgments This work was supported by a grant from the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquitin (Ub) has been considered as one of the most import
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In addition to the blockade of
2019-11-27
In addition to the blockade of airway smooth muscle contractions, CysLT1 receptor antagonists also exerted a potent anti-inflammatory effect at this level. The oral administration of MEN91507, Pranlukast, Montelukast, and Zafirlukast also produced a long-lasting inhibition of leukotriene D4-induced
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In conclusion high methylation levels
2019-11-27
In conclusion, high methylation levels of CDKL2 were observed both in HCC cell lines and tissues, which showed a negative association with mRNA expression. Moreover, treatment with demethylation agent in HCC cell lines could upregulate CDKL2 mRNA expression. The discovery of the epigenetic modificat
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In conclusion as illustrated in Fig
2019-11-26
In conclusion, as illustrated in Fig. 5G, in response to MNNG-induced DNA damage, PARP-1 appears to have dual roles in determining the cell fate in response to MNNG: PARP-1 activation is the cause of non-apoptotic cell death via ATP depletion and PARP-1 activation is able to elicit a self-protective
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br Results and discussion To check the
2019-11-26
Results and discussion To check the 88 3 that the charge of α-synuclein can be altered due to the glycation, we measured zeta potential of native α-synuclein and α-synuclein glycated by two different glycating agents, methylglyoxal (MG) and glyceraldehyde-3-phosphate (GA-3-P). The value for nativ
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Three dimensional conformational changes in the cargo
2019-11-26
Three-dimensional conformational changes in the cargo protein’s NES, caused by protein phosphorylation, dephosphorylation, or mutation, can regulate CRM1 binding (Craig et al., 2002, Vogt et al., 2005). Additional protein modifications such as sumoylation, ubiquitination, acetylation, and/or the bin
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benzbromarone The current study showed that the
2019-11-26
The current study showed that the tested nonselective COX inhibitors potentiated the neuronal (EFS) and endothelial (ACh)-dependent relaxation of rat corpus cavernosum. Indomethacin was the most effective among them in potentiating EFS-induced relaxation. Diclofenac was the most effective in potenti
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Damage of PE HD due to
2019-11-26
Damage of PE-HD due to both mechanisms is usually considered to emerge from a local stress concentration in the material, leading to the initiation of a crack, which subsequently propagates further through the material, and finally leads to macroscopic failure. In this process, crack growth occurs o
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The H E staining and Nissl staining results showed
2019-11-26
The H&E staining and Nissl staining results showed that damage to the pyramidal neurons in the CA1 and CA3 regions of the hippocampus were observed in the 50 mg/kg/day DBP group, accompanied by an absence of Nissl bodies, suggesting that DBP exposure can lead to pathological changes in the neurons o
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br Other pathways involved in the
2019-11-26
Other pathways involved in the preventive and therapeutic potential of flavonoids in neurodegenerative diseases Rather than the induction of MAPK/ERK pathway, flavonoids actively modulate other critical intracellular neuronal survival and death protein kinases pathways, more importantly PI3K/Akt,
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Importantly our in vivo data fit to the
2019-11-26
Importantly, our in vivo data fit to the in vitro data, further confirming the synergistic effect of XJD and gefitinib on the inhibition of lung cancer and the regulation of SP1, HOTAIR, and EP4 YC 1 receptor levels. The doses of XJD used were based on our previous in vivo study (Zhao et al., 2016)
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all trans retinoic acid Key molecules in the EP second messe
2019-11-26
Key molecules in the EP1 second messenger signaling cascade that are necessary for potentiation of GluK2/GluK5 were identified. We also identified three GluK5 serines located in a membrane-proximal C-terminal domain that, when mutated to the phosphomimetic aspartate and expressed with GluK2, rendere
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