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ERR and ERR share high sequence homology at
2020-02-28

ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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In conclusion we designed novel E
2020-02-28

In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and , we f
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A previous pharmacokinetic study of curcumin
2020-02-28

A previous pharmacokinetic study of curcumin in mice demonstrated that curcumin could not be detected in plasma after a single oral dose of 75 mg/kg of curcumin. After 4-months administration of 75 and 300 mg/kg of curcumin, plasma levels of curcumin and THC were 0.095 and 0.465 μM and 0.025 and 0.1
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Modulating protein stability specifically inhibiting ubiquit
2020-02-27

Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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This study demonstrates that GUL
2020-02-27

This study demonstrates that GUL-1 affects multiple pathways/processes. As GUL-1 is likely to function as an RNA-binding protein, it is conceivable that the mRNAs involved are bound to GUL-1 as part of the regulatory function of the protein. In fact, in S. cerevisiae Ssd1 was shown to bind multiple
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The importance of AAE in enhancing the survival of plants
2020-02-27

The importance of AAE3 in enhancing the survival of plants and yeast when confronted with certain environmental stresses has been documented in recent reports. In response to biotic stress such as oxalate-secreting micro-organisms, AAE3 was found to reduce the inhibitory growth effects of the secret
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mtor inhibitors While oxysterols were most extensively
2020-02-27

While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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Compounds that interact with MDR can do
2020-02-27

Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant lactone mg and there was no observed reduct
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Here we uncover a highly diverse superfamily of self replica
2020-02-27

Here we uncover a highly diverse superfamily of self-replicating MGEs, dubbed pipolins, which are present in three major bacterial phyla, as well as in mitochondria, and encode divergent PolB carrying TPR1 and TPR2 subdomains. Biochemical characterization of a representative enzyme encoded by a pipo
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In conclusion we have recombinantly expressed and purified t
2020-02-27

In conclusion, we have recombinantly expressed and purified the product of the YP_002262821.1 gene from A. salmonicida and confirmed that it possesses ATP-dependent DNA ligase activity. Comparison of the full-length and truncated versions of the protein indicate that the N-terminal 25 psora encode
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br Subjects and methods br Results
2020-02-27

Subjects and methods Results Discussion In the present study, we found significantly increased CSF levels of IL-4, IL-5, IL-9, IL-10, TNF-α, CXCL8/IL-8, and VEGF-A together with significantly higher detection rates of IL-6, GM-CSF, PDGF-BB and IL-1ra in IHP patients compared with OND patien
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Estradiol Compound was generated using a literature procedur
2020-02-27

Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to Estradiol ). Hydrolysis of all methyl e
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Boulares group has demonstrated that the NF B
2020-02-26

Boulares group [82] has demonstrated that the NF-κB1/p50 NF-κB, a family member of type I NF-κB, is an excellent substrate for DNA-PK, which-dependent phosphorylation of NF-κB1 at serine 20 appears to enhance its binding to DNA as either a homodimer or a heterodimer with p65 NF-κB and the ability of
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br Methods for assessing TLS
2020-02-26

Methods for assessing TLS While the precise quantification of restricted DNA synthesis events is possible (e.g. unscheduled DNA synthesis (UDS) reveals NER), so far, it is impossible to identify TLS stretches of only a few nucleotides within the background of bulk DNA replication of normal DNA. N
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A range of therapies exists for
2020-02-26

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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