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As illustrated in among all
2022-06-17
As illustrated in , among all synthesized compounds, biphenyl derivatives , , , , and with substitutions at the 3-position possessed the best FAAH inhibitory capacity. These 5 compounds demonstrated a good activity against FAAH with IC values in a submicromolar range. Nevertheless, when replacing th
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Although oxidative stress induces a decrease in
2022-06-16
Although oxidative stress induces a decrease in intracellular ATP level, the underlying mechanism is obscured. We hypothesized that oxidative stress induced by H2O2 could decrease astrocytes ATP level through lysosome exocytosis in Ca2+-dependent pattern. In present study, using H2O2 stimulation to
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Several studies have also shown that HK may be
2022-06-16
Several studies have also shown that HK2 may be an important downstream ApexBlue™ Quick Cell Viability Fluorometric Assay Kit of the PI3K/AKT/mTOR signaling pathway and may contribute to the development of cancer [15]. In our previous study, we found AKT2 expression was positively correlated with
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br Trifluoromethylketones This group of
2022-06-16
Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Urea in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif for th
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NCSs are helical proteins containing four EF
2022-06-16
NCSs are α-helical proteins containing four EF-hand motifs with EF1 being incapable of Ca-binding throughout the family (atomic-resolution structure was firstly resolved for recoverin [5]; for review on NCS structure, see [6]). Some of the NCS proteins (i.e. recoverin and KChIP3) have two while othe
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Ras pathways are involved in the regulation of
2022-06-16
Ras pathways are involved in the regulation of virulence in Cryptococcus neoformans [7] and Candida albicans [8,9]. To verify the importance of Ras in the survival response of the fungus in the host, a pathogenicity test of P. brasiliensis was performed before and after treatment with the Ras inhibi
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AP and NF B activation is inhibited by curcumin
2022-06-16
AP-1 [16], [17] and NF-κB activation is inhibited by curcumin (diferuloylmethane) [18], [19], the yellow component of Curcuma longa that gives curry its colour and flavour. Curcumin has shown anti-inflammatory and antioxidant properties [20], [21], [22], [23], [24], [25], [26] due to the inhibition
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A few methods have been developed to separate and
2022-06-16
A few methods have been developed to separate and prepare compounds from L. chinensis, such as silica gel column chromatography [5,6] and high-performance liquid chromatography (HPLC) [7]. Silica gel column chromatography is still used for its simple equipment and low cost. However, this method is o
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br Materials and methods br Results
2022-06-16
Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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SAR around amino derivative revealed a number of interesting
2022-06-16
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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Due to the high structural similarity between
2022-06-16
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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The aim of this study is to
2022-06-16
The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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In response to oxidative stress in
2022-06-16
In response to oxidative stress in DM, antioxidant defence systems are activated in β-cells. Glutathione (GSH) is one of the most abundant antioxidants and has been shown to be expressed at lower concentrations in patients with DM [12], [13]. Furthermore, plasma levels of glycine, which is a synthet
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Even with all of the subunits
2022-06-15
Even with all of the subunits present, the complex must also be correctly assembled for the enzyme to function properly. The complex is first assembled in the endoplasmic reticulum, with NCT and APH-1 binding together. They form the initial scaffold, so full-length PS can attach itself, and finally
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Michiel S van der Heijden had full access to
2022-06-15
Michiel S. van der Heijden had full access to all GZD824 receptor data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven. Wang,
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