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The combination of Aurora kinase inhibitors with standard ch
2024-06-04

The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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The Rv c EQ protein was purified
2024-06-04

The Rv2477c-EQ2 protein was purified from 600 ml induced cultures following the same protocol described above. Elution of the mutant protein from the affinity resin was done using 200 mM imidazole. After concentration and buffer-exchange of protein as described above, the purity of the protein was c
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Recent studies have indicated that V ATPase activity
2024-06-04

Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ CGP 53353 have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ cells' a
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In order to further explore whether the cytoprotective effec
2024-06-04

In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 regadenoson receptor is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A
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WKY and SHR strains have important
2024-06-04

WKY and SHR strains have important differences mainly in their sympathetic status but also in the activity of the RAS. The development of hypertension in SHR is clearly related to an increase in sympathetic activity [51], [11]. In addition, increased renal sympathetic nerve activity led to an increa
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Modulating the ability of tumor cells to
2024-06-03

Modulating the ability of tumor Olomoucine to detoxify ROS is a key mechanism by which cysteine metabolism affects tumor cell survival. One study observed hypermethylation of cysteine dioxygenase (CDO1) in 60% of tested breast cancer samples, leading to increased ROS detoxification and tumor cell s
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Di ethylhexyl phthalate DEHP is
2024-06-03

Di-(2-ethylhexyl) phthalate (DEHP) is one of the most widely used environmental chemicals in the production of polyvinyl chloride. After thapsigargin mg into human body, DEHP can be converted to the metabolite mono-ethylhexyl phthalate (MEHP), which has higher toxicity than DEHP and can influence r
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br Perspectives Given the complexity of the
2024-06-03

Perspectives Given the complexity of the cellular interactome and of protein scaffolding, further progress in revealing how individual membrane proteins, including APP and AChE, interact with each other at various levels, from cell-surface shedding to gene regulation, will clarify some intrinsic
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Having taken a step back from affinity
2024-06-03

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br Aurora A Aurora B
2024-06-03

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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br Materials and methods br Results
2024-06-03

Materials and methods Results Discussion Proteomics analyses generate mountains of data, expression information for hundreds or thousands of proteins in a single experiment (Wojcik and Schächter, 2000). Recently proteomics and bioinformatics provide new understandings about the processes in
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The levels of Mcl and FLIP are
2024-06-03

The levels of Mcl-1 and FLIP are homeostatically controlled by transcriptional and posttranslational processes. Accumulating evidence suggested that intracellular signaling molecules such as Akt are crucial to the transcription of Mcl-1 and FLIP [30], [31]. The constitutive activation of Akt is dete
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br Introduction Androgens have been shown to
2024-05-31

Introduction Androgens have been shown to regulate several neural functions ranging from reproduction to mood and cognitive abilities. This property starts as early as the perinatal period, which is characterized by prenatal and postnatal surges of gonadal testosterone, and continues through pube
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We have recently begun to demonstrate this concept
2024-05-31

We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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Recent work has detailed the impact of genetic deletion of
2024-05-31

Recent work has detailed the impact of genetic Naphthoquine phosphate of AMPK in the liver, revealing only minor phenotypes upon removal in mice (Boudaba et al., 2018). However, these studies very elegantly showed the potential for small molecule-mediated activation of AMPK to elicit large changes
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