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Three kinase inhibitors dasatinib type I imatinib type
2021-04-06
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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Most of the data indicating
2021-04-06
Most of the data indicating that the six-ankyrin repeat domain-containing Asb genes drive compartment expansion come from zebrafish and concern Asb11. However, there is evidence to suggest that these data can be expanded to the entire vertebrate phylum and to all six-ankyrin repeat domain-containing
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E ubiquitin ligases are key
2021-04-06
E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligases
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br Results br Discussion Many studies have
2021-04-06
Results Discussion Many studies have shown that intrinsic properties of the E2 enzyme govern the nature of the Ub modification, including both the multiplicity of the Ub modification and the specific KU-0060648 type in the case of polyubiquitin chains [3], [4], [9], [14]. Whereas previous stu
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Together the protein engineering approaches employed
2021-04-06
Together, the protein engineering approaches employed by Teyra et al., (2019) demonstrate the effectiveness of affinity maturation for improving the affinity of UbVs, but this comes at a cost in terms of specificity. Indeed, the most effective UbV was the dimeric construct generated from UbVs isolat
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Our western blotting results showed
2021-04-06
Our western blotting results showed that phospho-DDR1 levels continued to increase after I/R injury, and the overall activation trend between phospho-DDR1 and MMP-9 was the same. We found that phospho-DDR1 expression started to increase significantly at 12h after I/R injury, which may be related to
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Cell lines which possess microglial or neuronal properties a
2021-04-06
Cell lines which possess microglial or neuronal properties are uncomplicated and convenient in vitro models for studying cc-5013 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 a
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The CysLT receptor antagonist BayCysLT
2021-04-06
The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear latanoprost into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Barret et
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In our model CSF R blockade with
2021-04-06
In our model, CSF-1R blockade with PLX647 mainly targeted the more abundant MDSCs instead of macrophages, suggesting that the role of CSF-1 may be tumor model-dependent. Different tumor models, genetic backgrounds, or treatments may induce different growth factors or cytokines in the tumor microenvi
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Compound A and Compound B Fig were found
2021-04-06
Compound A and Compound B (Fig. 4) were found in our in vitro screening assays and have similar CRF1 receptor in vitro profiles (Table 1). When binding was investigated using [125I]-CRF in ex vivo assay, Compound A inhibited binding of [125I]-CRF both in the frontal cortex and the pituitary; however
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There are two general approaches to building Bayesian networ
2021-04-06
There are two general approaches to building Bayesian networks for the purpose of risk assessment. Researchers can implement static models that predict risk or survival at a snap-shot of time. For example, Loghmanpour et al. [10] created Bayesian network-based risk assessment models for patient data
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While previously reported optimizations on compound
2021-04-02
While previously reported optimizations on Etoricoxib focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore new ch
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We further assessed EBI expression in RRMS
2021-04-02
We further assessed EBI2 expression in RRMS patients before and during NTZ treatment. A significant increase of EBI2 expression was observed in memory CD4+ T cell subpopulations, but not in CD8+ T cell or in CD19+ B cell subsets of patients undergoing NTZ treatment, with a parallel gain in the migra
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In the SUMOylation pathway SCE as an E enzyme
2021-04-02
In the SUMOylation pathway, SCE1 as an E2 enzyme has an important role in mediating the conjugation of SUMO to target proteins. The accumulated SUMO conjugates in plants are associated with abiotic stress responses (Castro et al, 2012). We performed a drought stress analysis on WT plants, induced by
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Refametinib receptor Together the protein engineering approa
2021-04-02
Together, the protein engineering approaches employed by Teyra et al., (2019) demonstrate the effectiveness of affinity maturation for improving the affinity of UbVs, but this comes at a cost in terms of specificity. Indeed, the most effective UbV was the dimeric construct generated from UbVs isolat
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