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We recently employed a functional drug screening approach
2019-11-06
We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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The defining molecular feature of Ewing
2019-11-06
The defining molecular feature of Ewing sarcoma is the characteristic EWSR1/ETS fusion protein, most commonly involving EWSR1 and FLI1 (Delattre et al., 1992, May et al., 1993). EWS–FLI1 causes global changes in gene expression both by directly regulating gene expression and by causing changes in ch
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Our previous high throughput screening HTS campaign using
2019-11-06
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based 14520 milliliters to liters assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20
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Because macrophages clear the injured
2019-11-05
Because macrophages clear the injured tissue of dead plerixafor sale and matrix debris, macrophage infiltration is essential for normal tissue repair. In cardiac remodeling by MI, however, macrophages infiltrate excessively into not only the infarct area and marginal area of MI. Infiltrated macroph
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The UPR is composed of three
2019-11-05
The UPR is composed of three different pathways that fall under the control of three respective ER transmembrane proteins: PERK, IRE1α (inositol-requiring enzyme 1α) and ATF6 (activating transcription factor 6). As a starting signal for the UPR, misfolded proteins induce the release of GRP78 from th
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Compound was generated using a literature procedure
2019-11-05
Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to Gemcitabine ). Hydrolysis of all methyl
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Another well established visceral action of CRF
2019-11-05
Another well-established visceral action of CRF and urocortin administered peripherally is the long-lasting lowering of blood pressure observed in various species ranging from rodents to humans [22]. Existing evidence suggests that the hypotensive action of CRF and urocortin is mediated by the inter
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am580 Yet the standards fall back
2019-11-05
Yet, the standards fall back on the development process with justification. As shown by Littlewood and Strigini (1993), the extent to which the reliability of software (both OTS and bespoke) can be proved by testing is severely limited––not because appropriate tests cannot be devised, but because ad
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The combination of brequinar and fluorouracil FU has been
2019-11-05
The combination of brequinar and 5-fluorouracil (5-FU) has been evaluated to assess whether brequinar-induced uridine depletion would improve 5-FU activity. In cells, 5-FU is metabolized into FdUMP and inhibits thymidylate synthetase, which catalyzes the formation of thymidine monophosphate from deo
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The absorption rate of polyphenols into
2019-11-04
The PIK-III rate of polyphenols into the body is usually low. For example, the absorption rate of epigallocatechin gallate (EGCG), an active component in GP, is approximately 1% (Chen et al., 1997). To increase absorption of GP in the body, people have been increasing their intake of functional foo
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Experiment B CP during fear
2019-11-04
Experiment 4B: CP154,526 during fear acquisition normalizes fear-potentiated startle and prevents exacerbation of contextual conditioned fear in SERT−/− rats. As genotypes differed markedly in basal fear acquisition, drug effects could differ strongly between genotypes. Therefore, all effects in th
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br Conclusion In this work experiments were
2019-11-04
Conclusion In this work, experiments were carried out to purify the protein with COX activity, using an anti-mouse COX-2 pAb and a COX activity assay as tools for monitoring the protein responsible for this activity in the parasite. Gp63 enrichment through the affinity column and identification b
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br Introduction Al Awqati and his colleagues using R
2019-11-04
Introduction Al Awqati and his colleagues using R(+)-methylindazone, R(+)-[(6,7-dichloro-2-cyclopentyl-2,3-dihydro-2-methyl-1-oxo-1H-inden-5-yl)-oxy] acetic Quinacrine hydrochloride hydrate mg (IAA-94) (Landry et al., 1987) isolated the first chloride intracellular ion channel (CLIC) proteins (p
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SGX523 australia The H E staining and Nissl staining results
2019-11-04
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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821 br Effects of culture conditions
2019-11-04
Effects of culture conditions on drug-induced gene 821 in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that are most critical for
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