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Hymenialdisine the most potent inhibitor of parasite
2020-11-23

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this Methoxyresorufin also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of
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br Acknowledgements br Introduction Protein tyrosine
2020-11-23

Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th
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br Concluding remarks Some of the clinical trials of putativ
2020-11-23

Concluding remarks Some of the clinical trials of putative neutral competitive ERAs have been less successful than anticipated 6, 8, 11. This might be because of underestimation of the complexity of the molecular pharmacology of ETA. To resolve this, it will be necessary to define the signaling m
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The Ewing sarcoma breakpoint region gene EWSR is a
2020-11-20

The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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br STAR Methods br Acknowledgments We
2020-11-20

STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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Sennoside C Recent studies have reported that miR
2020-11-20

Recent studies have reported that miR-454 plays an important role in various cellular processes and diseases, such as inflammation, infection, osteogenic differentiation, and cancers [25,27,29,30]. Multiple evidence has documented that miR-454 promotes the proliferation, migration and invasion, and
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To further confirm the roles of
2020-11-20

To further confirm the roles of the CYP450 enzymes involved in the metabolism of Dip in rat liver microsomes, we utilized not only chemical inhibitors but also a correlation analysis and a panel of recombinant rat CYP450 enzymes to evaluate the contribution of CYP450 enzymes. The results of the corr
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Our studies approached this problem using integrative
2020-11-20

Our studies approached this problem using integrative -omics analysis of human NK-ieILC1s from distinct microenvironments and functional subsets, including helper and adaptive phenotypes. At both the transcriptional and epigenetic levels, we find that the adaptive subset, CD57+ cytotoxic NK cells, s
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While apparent that His Artemis fractionated over a HAP
2020-11-20

While apparent that [His]6-Artemis fractionated over a HAP column is devoid of 5′–3′ exonuclease activity but still retains DNA-PK dependent hairpin-opening activity, we sought to further assess DNA-PK dependent Artemis overhang cleavage activity to ensure all the in vivo, intrinsic enzymatic activi
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This project was funded by the Deutsche Forschungsgemeinscha
2020-11-20

This project was funded by the Deutsche Forschungsgemeinschaft within FOR 2251 (project grants EB 285/2-1 and WI 3272/3-1) and in part by additional contributions from the Bundesministerium für Bildung und Forschung (D.I.S award Nos. BIOSCAT [05K12YE1]) and the Horizon 2020 programme of the European
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Ion Channel Compound Library Analysis of Table shows that
2020-11-20

Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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9184 br Chagas disease and HAT drug R
2020-11-19

Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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Cell lines which possess microglial or
2020-11-19

Cell lines which possess microglial or neuronal properties are uncomplicated and convenient in vitro models for studying gap 0 injury at the cellular and molecular levels. Microglial BV-2 cells are derived from the immortalized mouse microglia and exhibit many of the morphological, phenotypical and
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The distorted geography on the
2020-11-19

The distorted geography on the number lines of many pre-service primary teachers in this study also highlights the need to provide them with strong visual models of negative numbers and their ordering. The evidence from Indri's interview is that some standard models of negative numbers (e.g., lendin
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By live imaging of GUL
2020-11-19

By live imaging of GUL-1-GFP, we observed the kinetics of aggregate movement within the cell. One of the marked characteristics of GUL-1-GFP cytosolic (but not nuclear-associated) aggregate motion was a “comet-like” movement that was found to be dependent on the presence of properly polymerized micr
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