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Molecular docking quantitative structure activity
2023-08-01
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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The protein kinase CK mediated phosphorylation of HMGN was
2023-08-01
The protein kinase CK2-mediated phosphorylation of HMGN1 was implicated to be involved in age-associated amnesia in rats [31]. It was shown that the decreased level of HMGN1 phosphorylation due to the down-regulation of CK2 activity could cause amnesia in aged rats, whereas the treatment with protei
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Aconitase clusters are prone to oxidations and are among
2023-08-01
Aconitase clusters are prone to oxidations and are among the first to undergo a change in transition state during stages of electrophilic stress rendering them inactive [31]. Aconitase activity in LETO and OLETF did not differ at T0 suggesting that the early onset of insulin resistance may not be at
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br Experimental procedures br Results br
2023-08-01
Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific
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To elucidate this relationship we developed
2023-08-01
To elucidate this relationship, we developed a spatial model of Ca-influx through N-methyl-D-aspartate receptor (NMDAR), CaMKII/PP1 activation, and AMPAR insertion in a realistic spine geometry. Using this model, we show that i) variables in membrane voltage mediated Ca-influx, particularly the numb
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Another class of AMPK regulator is peptidyl prolyl cis trans
2023-08-01
Another class of AMPK regulator is peptidyl-prolyl cis/trans isomerase (PPIase) NIMA-interacting 1 (Pin1), which binds to a number of proteins and regulates oncogenesis and metabolic diseases (Khanal et al., 2013; Zhou and Lu, 2016). Pin1 has been shown to bind to and inhibit AMPK; therefore, at lea
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Furthermore to address the concern that the
2023-08-01
Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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Regenerative mechanisms often require reemployment of
2023-08-01
Regenerative mechanisms often require reemployment of pathways used during development in the embryonic and postnatal periods (Waschek, 2002). PACAP has diverse neurodevelopmental and growth factor-like effects (Botia et al., 2007; Vaudry et al., 2009; Waschek, 2002; Watanabe et al., 2016) and it is
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br Thymic expression of AChR Both
2023-07-31
Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid follic
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Accumulating data suggest that ROS trigger
2023-07-31
Accumulating data suggest that ROS trigger autophagy but, in turn, autophagy reduces ROS levels [23]. Our results are in agreement because 27-OH mediated autophagy induction interms of LC3 II formation and Beclin 1 protein expression was suppressed by treating the promonocytic cells with the antioxi
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CHK has been reported to
2023-07-31
CHK1 has been reported to be the kinase responsible for H3.3S31 phosphorylation in human ALT cancer UCM05 australia . However, in our study, knockdown of CHK1 in HEK293F (Figs. S1c and S6) or HeLa S3 (data not shown) cells did not result in a significant decrease in H3.3S31ph, which is in agreement
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AP activation is known to upregulate
2023-07-31
AP-1 activation is known to upregulate downstream target genes including IL-4, murine recombinant australia D1, c-myc, Bcl-xl, MMP-9, EGFR, and specific miRNAs that are involved in progression and metastasis of tumors. Moreover, matrix metalloproteinase-2 has been shown as a downstream gene of AP-1
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ATM dependent initiation of radiation induced G M checkpoint
2023-07-31
ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or 4-DAMP with a kinase inactive allele of ATR (ATRkd) to evaluate the ro
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For the TSH receptor signaling at the Golgi trans Golgi
2023-07-31
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as NPPB depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continued signaling
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Analysis of ASK crystal structures as well
2023-07-31
Analysis of ASK1 crystal structures as well as an investigation of how ck1 inhibitor 4 might bind were undertaken to understand opportunities for engaging Gln756. To this end a docking model derived from PDB 3VW622 was used to predict the binding mode of amide 4 in the ASK1 active site as shown in
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