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Taken together these assays demonstrate
2020-06-10
Taken together, these assays demonstrate that SUMOD positioning is essential for all E3 ligases but dispensable for E2 and S*E2 sumoylation reactions. Thus, we propose SUMOD positioning as a key criterion to describe the enzymatic function of SUMO E3 ligases that distinguishes them from other enhanc
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br Discussion The biochemical separation of exonuclease acti
2020-06-10
Discussion The biochemical separation of exonuclease activity from DNA-PK dependent endonuclease activity reported in this manuscript is consistent with genetic separation of Artemis enzymatic activity. Mutations in the protein which result in disruption of endonuclease activity have no effect on
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pak4 Western blotting and flow cytometry was employed to ass
2020-06-10
Western blotting and flow cytometry was employed to assess the DNA-PK inhibition of LTU28 and LTU31 in combination with radiation. It has been previously reported that phosphorylation of DNA-PKcs at the Thr2609 cluster plays an important role in DSB repair and resistance to radiation (Ding et al., 2
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A range of therapies exists for the treatment of inflammatio
2020-06-10
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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Cisplatin The results showed that ethanol
2020-06-10
The results showed that ethanol and acetaldehyde production was not affected by the presence of CPA-7. We observed that the concentration of ethanol increased throughout the assay up to 95–179 μL L-1 regardless of the treatment. The acetaldehyde concentration reached its highest values after 6–9 day
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All known vertebrate TRIMs are
2020-06-09
All known vertebrate TRIMs are categorized in 11 distinct subclasses depending on the types of domains present at their carboxyl-terminals (Fig. 3) [29], [35]. Beyond conserved N-terminal domains, it is the C-terminal that provides specificity of interactions with other proteins. The subclass IV for
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In the past few years we
2020-06-09
In the past few years we and others have reported that GLP-1 may also be secreted by sub-populations of alpha E-64 in human pancreatic islets (Marchetti et al., 2012, Ellingsgaard et al., 2011), which could contribute to beta cell function and survival (Marchetti et al., 2012, Ellingsgaard et al.,
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br Acknowledgments br The design
2020-06-09
Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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ARA metabolites which are produced through cytochrome P CYP
2020-06-09
ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic Cy5 NHS ester(Et) (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and naturetic in the kidney
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In rats exposed to day of nicotine withdrawal
2020-06-09
In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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This structure guided the variation of the compounds aiming
2020-06-09
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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br Acknowledgments br Casein kinases CK are serine threonine
2020-06-09
Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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Given its high frequency it
2020-06-09
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant Moxidectin to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been prove
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Endothelial dysfunction has been associated with most of the
2020-06-09
Endothelial dysfunction has been associated with most of the established cardiovascular risk factors, such as hypercholesterolemia, hypertension, smoking, diabetes mellitus, a positive history of premature CAD and elevated Immunology Compound Library homocysteine 4, 26, 27. Endothelial dysfunction
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Research done thus far supports the hypothesis that MPA
2020-06-09
Research done thus far supports the hypothesis that MPA has detrimental effects on cognition, alone and in combination with estrogen; there are other FDA-approved progestogens that satisfy the uterus opposing effects that have not been cognitively profiled. An important goal to aid women\'s health i
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