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The possibility that a carboxyl group attached to the
2019-10-14
The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a
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Overall the DDR kinase domain has a typical
2019-10-14
Overall, the DDR1 kinase domain has a typical kinase domain structure and adequate sequence and/or structure similarity with other kinase domains, as shown in Fig. 2, which allow homology modeling of the active and inactive conformations. In addition to conformational changes to the activation loop
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Here we describe a novel series of arylazoderivatives develo
2019-10-14
Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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Colony stimulating factor receptor CSF R or cFMS
2019-10-14
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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br Results br Discussion MSCs derived
2019-10-12
Results Discussion MSCs derived from the bone marrow and adipose tissue have been shown to promote the growth and metastatic ability of breast cancer and other human malignancies, but the mechanisms are incompletely understood (Barcellos-Hoff et al., 2013, Cuiffo et al., 2014, Del Pozo Martin
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Taken together our results demonstrate
2019-10-12
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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As for the molecular mechanism Ferguson BD suggested that
2019-10-12
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of Taxifolin with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with high EphB4 expression levels
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Future advances in the in vivo molecular imaging of
2019-10-12
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measur
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Introduction In vitro synthetic biology has received conside
2019-10-12
Introduction In vitro synthetic biology has received considerably less attention than in vivo processes so far (Foster and Church, 2007). However, cell-free biosynthetic production is very likely to become important for many biotechnological challenges for reasons such as (energy) efficiency, syste
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In general we observed that the enolase gene with highest
2019-10-11
In general, we observed that the enolase gene with highest mRNA levels was TVAG_043500, under all three iron concentration conditions. mRNA levels for this gene are very similar in normal and iron rich cultures (73.9 and 78.1 fold change, respectively), and higher in iron depleted cultures (118.3 fo
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We not only found that the
2019-10-11
We not only found that the ISR leads to attenuation of conventional cap-dependent translation with no change in RAN translation of the G4C2 expanded repeat, but also that GA translation from the expanded repeat (but not from 5 G4C2 repeats, perhaps because the protein product does not aggregate) is
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Our study found a significant association between the degree
2019-10-11
Our study found a significant association between the degree of primary tumor lobulation and EGFR mutations status (P Galanthamine status. However, only a small portion of these previous studies included the evaluation of lobulation, and almost all of them reported no association between EGFR mutat
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A study profiling chemokine expression in LCLs revealed high
2019-10-11
A study profiling chemokine expression in LCLs revealed high expression levels of CCR6, CCR7, and CCR10 and low expression of CXCR4 and CXCR5 in EBV immortalized cells. Accordingly, LCLs showed a markedly increase in migration in response to the ligands of CCR6 (CCL20), CC7 (CCL21), and CCR10 (CCL28
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Terazosin clinical E ligases provide substrate recognition s
2019-10-11
E3 ligases provide substrate recognition specificity Ubiquitination Terazosin clinical and substrate specificity in mammals is achieved by the existence of over six-hundred E3-ubiquitin ligases that catalyze the final step of ubiquitination, compared with only one E1 and very few E2 enzymes known
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br Results br Discussion The ubiquitin system
2019-10-11
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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