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br Materials and methods br Acknowledgements
2020-03-23

Materials and methods Acknowledgements SD was supported by a pre-doctoral research fellowship from the Flanders Agency for Innovation and Entrepreneurship (VLAIO-Flanders, Belgium). YB is supported by a postdoctoral fellowship from Research Foundation Flanders (FWO, Belgium). We thank Isabell
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Previously to detect CDKL activity we used a
2020-03-23

Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti
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Previous studies from our laboratory in CD
2020-03-23

Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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By using the C elegans Matrisome Annotator
2020-03-23

By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome endothelin receptor antagonist in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elega
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The in vivo IC M
2020-03-23

The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free 221 2
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Drug drug interactions are frequently attributed
2020-03-23

Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is tho
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We have previously disclosed the
2020-03-23

We have previously disclosed the discovery of a 7-azaindole-3-acetic HA14-1 australia CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that
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We recently reported that the information about the electron
2020-03-21

We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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We hypothesize that both IGF dependent kinase
2020-03-21

We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal GSK2334470 mg in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies beca
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Upon Edn ligand binding endothelin receptors can induce a va
2020-03-21

Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example
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br Perspective and conclusion Collagen Toolkits II and
2020-03-21

Perspective and conclusion Collagen Toolkits II and III have been used to determine the flavopiridol for DDR1 and DDR2, and the main binding site is the GVM-GFO motif [103,108]. The co-crystal structure of the DS domain of human DDR2 bound to a synthetic collagen-like peptide containing the GVM-
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Oysters belong to the second largest animal
2020-03-21

Oysters belong to the second largest animal phylum Mollusca, and they are globally distributed aquaculture animals (Wang et al., 2018). A number of studies have demonstrated that oysters have evolved an integrated and complex innate immune system to recognize and eliminate various invaders. An array
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We neither observed changes in midazolam eCLmet indicative o
2020-03-21

We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/
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Redundancy of tumor promoting signaling pathways is
2020-03-21

Redundancy of tumor promoting signaling pathways is one of the mechanisms that prevent a lasting effect of targeted therapies, as has been demonstrated by the growing number of alternative pathways that confer resistance to EGFR-targeted therapies [3]. We show here that CSF-1R can, at least partiall
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In the present study we did not examine whether
2020-03-21

In the present study, we did not examine whether the CpG site-specific COMT methylation are associated with any genetic variants in response to E2, GEN or SFN. Some studies suggest that oxidative DNA damage causes genetic variation which may induce epigenetic changes that lead to gene silencing (Kho
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