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Our current understanding of nucleotide metabolism in
2020-01-08
Our current understanding of nucleotide metabolism in has made it possible to identify numerous proteins which serve essential roles in the life cycle of the parasite. One such protein is thymidylate synthase-dihydrofolate reductase (TS-DHFR), a bifunctional enzyme which is necessary for the product
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Drug drug interactions are frequently attributed to function
2020-01-08
Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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Collectively these data suggest the potential
2020-01-08
Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone\'s effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced
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In mouse lung arsenite enhances the formation
2020-01-08
In mouse lung, arsenite enhances the formation of cigarette smoke-induced 8-oxodeoxyguanine (Hays et al., 2006) and BaP-induced DNA adducts (Evans et al., 2004). Moreover, arsenite inhibits the repair of BaP-induced DNA adducts in human lung carcinoma A549 PJ34 (Schwerdtle et al., 2003), indicating
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We further analyzed the transcriptional mechanisms underlyin
2020-01-08
We further analyzed the transcriptional mechanisms underlying the synergistic action of IL-23 and PGE2 and found that this action is mediated by not only STAT3 but also CREB1 and NF-κB. Involvement of CREB1 is analogous to that in the PGE2-EP2/EP4–mediated Il12rb2 induction during TH1 cell different
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br Disclosure statement br Acknowledgment This
2020-01-08
Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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br Target enzyme attributes and substrate peptide selection
2020-01-08
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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Another potential source of variable affinities is
2020-01-07
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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br Conclusion The results of the present study
2020-01-07
Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by CysL
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CYP A is involved in the metabolism of
2020-01-07
CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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br Material and methods br
2020-01-06
Material and methods Results Discussion Both progesterone and estradiol are major ovarian steroids crucial for the development and homeostasis of the female reproductive tract (Patel et al., 2015). In the cervix, estrogen softens the cervical stroma affecting the extracellular matrix (ECM)
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Enhanced oxidative stress has been suggested as the critical
2020-01-06
Enhanced oxidative stress has been suggested as the critical mechanisms of IS-produced muscle damage [41,42]. NAC as a direct reactive oxygen species ROS scavenger is frequently discussed in the clinical trials of radiocontrast-induced AKI prevention [43]. Despite some supportive epidemiological dat
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br Other pathways involved in
2020-01-06
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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Interest in the PGE EP pathway is increasing given
2020-01-06
Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing BMS-650032 inflammation [15]. The EP4 rece
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DDR although normally expressed in cells with mesenchymal fe
2020-01-06
DDR2, although normally expressed in cGMP Dependent Kinase Inhibitor Peptide with mesenchymal features, has also been reported to enhance EMT. In A549 lung cancer cells, TGFβ1 increases the expression of type I collagen and DDR2. Knocking-down COL1A1 or DDR2 with siRNA is sufficient to inhibit EMT
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