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We recently employed a functional drug screening approach to
2021-03-10
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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We obtained two bands in RT PCR for
2021-03-10
We obtained two bands in RT-PCR for detection of SERPIN1-FOSB fusion when Taq DNA polymerase was used (Fig. 3A). Genuine RT-PCR product of SERPIN1-FOSB fusion was proved to be the shorter one (733 Phos-tag pairs) by sequencing, and the longer band (863 base pairs) was shown to be derived from nativ
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Our previous high throughput screening HTS campaign
2021-03-10
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based endothelin receptor antagonist assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations
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It is known that cigarette smoke increases the oxidative bur
2021-03-10
It is known that cigarette smoke increases the oxidative burden in the lungs of mice with emphysema, which leads to oxidative stress [[34], [35], [36]]. However, in addition to cigarette smoke, studies have shown that endogenous oxidative stress is associated with proteolytic MK-0457 in several mous
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Moreover Hypericum perforatum L was also included
2021-03-10
Moreover, Hypericum perforatum L. was also included in the initial screening, showing only a weak percentage of inhibition on both enzymes. In fact, it was not selected among the most active plants. The phytochemical profiles of these three Hypericum species were already reported to be significantly
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br EBV BILF A Virus Encoded TM
2021-03-10
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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Introduction Cognitive impairment is a core
2021-03-09
Introduction Cognitive impairment is a core, stable feature of schizophrenia that limits patient functioning and well-being (Keefe and Harvey, 2012) and associates with poor functional outcome (Fervaha et al., 2014, Kontaxaki et al., 2014). Studies also indicate that cognitive deficits occur prior
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Our data supports the conclusion that the exonuclease activi
2021-03-09
Our data supports the conclusion that the exonuclease activity thought to be intrinsic to Artemis is not a component of the Artemis polypeptide. Many possibilities exist to explain the presence of the exonuclease activity in less-pure fractions of Artemis. It is possible that the exonuclease is simp
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br Enzymes involved in microbial steroid
2021-03-09
Enzymes involved in microbial steroid degradation are generally not expressed constitutively, but they are upregulated depending on which steroid substrates are present [17,81]. Thus, a cell-free extract prepared from testosterone-adapted C. testosteroni ATCC 11996 cells displayed a 1(2)-dehydroge
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br Material and methods br Results br Discussion In vitro
2021-03-09
Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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br Acknowledgements We thank A Devia
2021-03-09
Acknowledgements We thank A. Devia-Barros and S.A. Barrios Latorre for invaluable technical support during the collection, maintenance and exposure of oysters. We are, furthermore, grateful to the municipal marina of Santa Marta for authorizing access to their facilities and to A. Franco for faci
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The four other mutations S
2021-03-09
The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels
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br Structure and function of EPAC
2021-03-09
Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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The following are the supplementary data related to this art
2021-03-09
The following are the supplementary data related to this article. Acknowledgments Introduction Cyclooxygenases metabolize arachidonic bcr-abl inhibitor to five primary prostanoids, PGE2, PGF2, PGI2, TXA2 (TX), and PGD2. These lipid mediators interact with specific members of a family of dist
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The acid base properties of the IL are important
2021-03-09
3. The acid-base properties of the IL are important issues to consider because protonation changes caused by Brønsted-acidic or basic ions may result in enzyme deactivation [29]. Thereby, the acid-base properties of the newly designed IL need proper control for enzymes by selection of appropriate ca
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