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Exposure to ultraviolet radiation with sunlight is
2020-03-03

Exposure to ultraviolet radiation with sunlight is generally accepted as the major cause of basal-cell carcinoma (Gallagher et al., 1995). The risk of this disease is significantly increased by age. Skin cancers are the most common tumours of the head and neck region and their prevalence shows progr
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br Results br Discussion Our
2020-03-03

Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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The cpm corresponding to bound substrate in
2020-03-02

The cpm corresponding to bound substrate in the sample well can be expressed as the difference between the total cpm in the sample well (3Hswtotal; 14Cswtotal) and the cpm for the unbound substrate in the sample well, as illustrated by Eq. (2): By combining Eqs. (1), (2), cpm for the bound substrat
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Next we compared the protease specificity of viruses NS
2020-03-02

Next, we compared the protease-specificity of viruses NS116-GFP/AE and NS116-GFP/AT for trypsin, neutrophilic elastase or supernatant of human neutrophils. For later purposes, we determined the viral yield in a co-cultivation system of infected Vero Nitrocefin with human neutrophils. The NS116-GFP/
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Experiments on the rat model of E coli pyelonephritis
2020-03-02

Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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Studies also provide evidence that cytokines such as TGF a
2020-03-02

Studies also provide evidence that cytokines such as TGF-β, a TH3-type cytokine, may also play a role in airway remodeling. Data obtained by Cohen et al suggest that TGF-β1 can induce human BSMC proliferation by increasing the expression of IGFBP-3. Hence, the mitogenic action of TGF-β1 could be rel
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Other studies have investigated the role of HDAC
2020-03-02

Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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To understand the behavior of enzymes in
2020-03-02

To understand the behavior of enzymes in ILs at a molecular level, it is first desirable to dissolve enzymes in the solvents. For soluble catalysts, there are many relatively simple spectroscopic and other techniques for obtaining accurate information at a molecular level. Parker et al. [9] reported
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Several main strategies for targeting
2020-03-02

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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Since both the Ub and ISG
2020-03-02

Since both the Ub and ISG15 systems are crucial for the innate immune response, many prokaryotic and viral pathogens have evolved ways to hijack them in order to create a “window-of-opportunity” for efficient replication. Several viral and bacterial proteins have been found to directly target these
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alzheimer\'s association Two are the sigma receptors ide
2020-03-02

Two are the sigma receptors identified to date: the non-opioid receptor, σ1R, and σ2R, whose identity with the Progesterone Receptor Membrane Component 1 (PGRMC-1) protein is in doubt (Chu et al., 2015). Despite endogenous ligands have not been yet identified, drugs of abuse may interact with these
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br Rationale and hypothesis To discover an allosteric
2020-03-02

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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In the context of E ligase drug discovery it
2020-03-02

In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 ZLN
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Consistent with a clear separation of biological
2020-03-02

Consistent with a clear separation of biological function between ARISC and BRISC in cells, mutations in BRCC36 and Abraxas are prevalent in cancer genomes whereas mutations in KIAA0157 are rare. A survey of the Catalogue of Somatic Mutations in Cancer (COSMIC) consortium, revealed that to date, 37
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Herein in continuation of our interest
2020-03-02

Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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