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The attachment of ubiquitin to RTKs such as EGFR
2021-02-26
The attachment of ubiquitin to RTKs, such as EGFR, mediates efficient delivery through the endosome-lysosome system for proteolysis. In this way, RTK degradation enables cessation of signal transduction. A recent siRNA screen identified a number of USPs that can significantly modulate EGFR levels an
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A structural explanation for how RBR RING
2021-02-26
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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Herein the interactions of etamicastat
2021-02-26
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the Dioscin exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains
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A second advance came with the discovery that conformational
2021-02-26
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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Introduction Maintenance of genome integrity is
2021-02-25
Introduction Maintenance of genome integrity is essential for life, and faithful DNA replication and repair ensure this. One of the most important parameters for DNA maintenance is the regulation of optimal concentrations of the four 5′-deoxyribonucleoside-triphosphates (dNTPs) the precursors for D
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In summary these results are consistent with our
2021-02-25
In summary, these results are consistent with our hypothesis that chemical nitrosation of BMAA to N-BMAA results in the formation of an alkylating agent. Furthermore, we have shown that N-BMAA is more toxic than BMAA itself. Previously, methylazoxymethanol (MAM), which is also present in the cycad n
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In the present study we used a new luminescent method
2021-02-25
In the present study, we used a new luminescent method to measure CYP activity with Luciferin-ME as a substrate which is used for wide ranges of mammalian CYPs, including CYP1A2, CYP2C8, CYP2C9, CYP2J2, CYP4A11, and CYP4F3B. As a result, no significant modulations of CYP activities in B[a]P exposure
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Since free testosterone diffuses into a
2021-02-25
Since free testosterone diffuses into a target organ [1], a remarkable increase in free testosterone in plasma is expected to enhance androgen response in target organs including the prostate. In fact, the results of the present study showed testosterone and DHT levels, and mRNA expression levels of
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Building applications by selecting and integrating component
2021-02-25
Building applications by selecting and integrating components is known in software engineering as COTS-based development. Nowadays, this approach is recognized as a crucial success factor for the software industry (Ahuja, 2014). The advantages of using COTS components include minimizing the overall
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Present study observed failure of PPE usage by the majority
2021-02-25
Present study observed failure of PPE usage by the majority of workers, which may be notable problem and may create a significant health effects due to pesticide exposure. Non-usage of PPE and its ill effects have been reported among farmers in Brazil [24,25] and Nepal [26]. It was reported that use
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br Roles of ERR in Physiology and Disease
2021-02-25
Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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Repulsive interactions towards undesirable substrates are ar
2021-02-25
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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To function as Ub ligases E proteins
2021-02-25
To function as Ub-ligases, E3 proteins must interact with E2s. As compared to the extensive studies on E3s, functional studies on E2s are relatively rudimentary in higher plants. We previously reported that there are 48 genes encoding Ub-conjugating (UBC) fold-containing putative E2 proteins in the
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Based on our studies presented
2021-02-24
Based on our studies presented above, atipamezole can be used as a new in vitro and in vivo tool Calcitriol as a pan-CYP inhibitor for CYP mediated metabolism study. It carries many unique characteristics compared to ABT which is currently being widely used for this purpose. These new characteristi
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br Results On the th day
2021-02-24
Results On the 8th day, the horizontal (Fig. 1) and vertical locomotor activity (Fig. 2) and the dorsal (Fig. 3) and BQ-788 sodium salt striatal dopamine release (Fig. 4) increased significantly in nicotine-treated rats, compared with the saline-treated rats. Tukey post-hoc test revealed the fol
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