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More than thirty enzymes with PLA activity have been describ
2019-12-02
More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos
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Dual inhibition of ACE and NEP as a
2019-12-02
Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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ion channels The secondary objective of the present study
2019-11-30
The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do
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Alvocidib flavopiridol is a piperidine chromenone
2019-11-30
Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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Previous studies on the chemokines role in depression are
2019-11-30
Previous studies on the chemokines role in depression are not detailed enough, and cannot sufficiently demonstrate even a hypothetical mechanism explaining the differences in levels of particular chemokines and their receptors, in relation to the severity of depression [29], [30]. Previous studies o
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Colony stimulating factor receptor CSF
2019-11-30
Colony stimulating factor-1 receptor (CSF-1R or cFMS) is a type III receptor tyrosine kinase. It is activated by binding with CSF-1 and IL-34, which stimulates differentiation, proliferation, survival and migration of monocyte-macrophage lineage cells., , , Also, macrophages produce inflammatory me
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Interestingly ASV infusion in the dRN of
2019-11-30
Interestingly, ASV-30 infusion in the dRN of saline pre-treated rats had no effect on anxiety-like behaviors. This result may be due to the saline pre-treated group exhibiting relatively low levels of anxiety-like behaviors (when compared to saline pre-treated rat of the first experiment that were n
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Another question concerns the mechanism of PC reduction duri
2019-11-30
Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens
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The in vitro cytotoxicity of
2019-11-30
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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br Materials and methods br Results and discussion br
2019-11-30
Materials and methods Results and discussion Conclusions In this study, we have investigated the possibility that hierarchical phosphorylation by CK2 may play a role in cellular signal transduction. Hierarchical phosphorylation by CK2 requires multiple consensus determinants with specific s
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br Materials and methods br Data and
2019-11-30
Materials and methods Data and statistical analysis The results were expressed as mean ± SEM. One-way analysis of variance (ANOVA), followed by Bonferroni\'s post-test or unpaired Student\'s t-test were used to determine significant differences between groups. The program used for statistical
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All tested antibodies exhibited positive immunoreactivity in
2019-11-30
All tested JQ1 exhibited positive immunoreactivity in NSCLC tumors, with N’-epitope being the less expressed (both as overall positivity and number of positive cases, or intensity combined with number of positive cells, as provided by H-Score. This result is in accordance with previous studies [18]
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Functional studies revealed that these
2019-11-30
Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea
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fluoxetine hydrochloride br In order to determine the physio
2019-11-30
In order to determine the physiological roles of WT (wild type) EWSR1, Dr. Lee\'s group established a conventional Ewsr1 KO mouse [38]. Since then, the Ewsr1 KO (−/−) mouse model has successfully been utilized to decipher many important in vivo roles of EWSR1 (Fig. 1). EWSR1 deficiency alters m
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While previously reported optimizations on
2019-11-30
While previously reported optimizations on (Z)-4-Hydroxytamoxifen mg focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B ()
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