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The synthesis of compounds a and
2021-07-28
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of mps1 kinase 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were
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br Introduction Biocatalysis can be used
2021-07-28
Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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Cysteinyl leukotrienes CysLTs are potent inflammatory
2021-07-28
Cysteinyl leukotrienes (CysLTs) are potent inflammatory mediators closely associated with cerebral ischemic injury. CysLTs induce inflammatory responses mediated by at least two different CysLT receptors (CysLT1R and CysLT2R) (Bäck et al., 2011, Singh et al., 2010). It has been reported that the Cys
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Introduction Quassinoids are natural products formed through
2021-07-28
Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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Previously to detect CDKL activity we used a radioactive pho
2021-07-28
Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti
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Nuclear export mediated by CRM is initiated by
2021-07-28
Nuclear export mediated by CRM1 is initiated by an interaction between RanGTP and the HEAT9 loop of CRM1, triggering a conformational change in the NES binding site that permits NES–cargo protein binding (Dong et al., 2009, Fung and Chook, 2014). Our docking simulation results predicted that DP2392-
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Acknowledgments The authors thank Dr
2021-07-27
Acknowledgments The authors thank Dr. Vladimir Poltoratsky and Zhihui Xiao for their help with the in vitro FRET assay. Support for this research was provided by Saint John’s University. Introduction We predicted the existence of endothelium-derived contractile factors (EDCFs) in 1982 [1]. In 1
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IGF-1, human recombinant The inhibition of CYP activity by N
2021-07-27
The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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The use of recombinant ER and ER binding assays
2021-07-27
The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct ARCA EGFP mRNA receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein production system
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In addition to the ESIs identified that target both
2021-07-27
In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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br Materials and methods br Results and
2021-07-27
Materials and methods Results and discussion Concluding remarks Enzymatic production of bioactive 9-cis-11-trans-conjugated linoleic prostaglandin receptor is part of a detoxification mechanism against linoleic acid which is a toxic and stress factor for many lactic bacteria such as Lactob
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For most enolases fluoride acts
2021-07-27
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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In our opinion the precise function of AE of
2021-07-27
In our opinion, the precise function of AE of S. mansoni (Sm32) remains unclear, and accurate knowledge of the three dimensional structure of this enzyme would be valuable for a better understanding the molecular basis of many of its properties, including its role in the host-parasite interaction, a
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Pursuant to our in vitro
2021-07-27
Pursuant to our in vitro data that neutrophilic elastase activated the elastase-dependent oncolytic virus, we initially hypothesized that tumor-infiltrating neutrophils could be the source for elastase in tumor tissue. However, we did not detect neutrophils in the PANC-1 tumor tissue where we observ
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To get an indication whether
2021-07-27
To get an indication whether GBM-derived 25-OHC could act as a chemotactic signal for monocytes, lipid extracts of GM133 media were used in THP-1 migration assays. Although an indirect approach, these experiments revealed that medium lipid extracts induced monocyte migration in a quantitatively comp
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