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1.
The G protein-coupled receptor GPR183/EBI2, which is activated by oxysterols, is a therapeutic target for inflammatory and metabolic diseases where both antagonists and agonists are of potential interest. Using the piperazine diamide core of the known GPR183 antagonist (E)-3-(4-bromophenyl)-1-(4-(4-methoxybenzoyl)piperazin-1-yl)prop-2-en-1-one (NIBR189) as starting point, we identified and sourced 79 structurally related compounds that were commercially available. In vitro screening of this compound collection using a Ca2+ mobilization assay resulted in the identification of 10 compounds with agonist properties. To enable establishment of initial structure-activity relationship trends, these were supplemented with five in-house compounds, two of which were also shown to be GPR183 agonists. Taken together, our findings suggest that the agonist activity of this compound series is dictated by the substitution pattern of one of the two distal phenyl rings, which functions as a molecular efficacy-switch.  相似文献   
2.
In the present study, 17 wt % TiN reinforced α-β SiAlON composites were sintered at low temperature by susceptor-assisted microwave heating. The effect of TiN addition on dielectrical properties of starting powders, as well as the influence of sintering temperature on phase evolution, microstructure development and mechanical properties of α/β-SiAlON-TiN composites were investigated. The obtained results showed that TiN addition increased the microwave absorbing properties which is reflected in the peak sintering temperature. Thus, the α:β ratio decreased and mechanical properties were improved, especially the fracture toughness of the composites. Furthermore, an estimate of energy consumption during microwave assisted sintering at the laboratory scale is presented. As a result, the highest values for relative density (97.1%), Vickers hardness (13.35 ± 0.47 GPa), and fracture toughness (7.52 ± 0.54 MPa m1/2) were obtained by microwave sintering for 30 min at 1300 °C.  相似文献   
3.
The substantial increase in DNA sequencing efforts has led to a rapid expansion of available sequences in glycoside hydrolase families. The ever-increasing sequence space presents considerable opportunities for the search for enzymes with novel functionalities. In this work, the sequence-function space of glycoside hydrolase family 94 (GH94) was explored in detail, using a combined approach of phylogenetic analysis and sequence similarity networks. The identification and experimental screening of unknown clusters led to the discovery of an enzyme from the soil bacterium Paenibacillus polymyxa that acts as a 4-O-β-d -glucosyl-d -galactose phosphorylase (GGalP), a specificity that has not been reported to date. Detailed characterization of GGalP revealed that its kinetic parameters were consistent with those of other known phosphorylases. Furthermore, the enzyme could be used for production of the rare disaccharides 4-O-β-d -glucosyl-d -galactose and 4-O-β-d -glucosyl-l -arabinose. Our current work highlights the power of rational sequence space exploration in the search for novel enzyme specificities, as well as the potential of phosphorylases for rare disaccharide synthesis.  相似文献   
4.
Wireless Networks - Nowadays, Wireless Sensor Networks are one of the fundamental infrastructures for IoT technology. Although WSN has been researched for a decade, providing energy efficiency for...  相似文献   
5.
In the presented study, the structural, thermal, and mechanical properties of the nanocomposites were investigated by doping silanized hexagonal boron carbide (h-B4C) nanoparticles in varying proportions (0.5%, 1%, 2%, 3%, 4%, and 5%) into the epoxy resin by weight. For this purpose, the surfaces of h-B4C nanoparticles were silanized by using 3-(glycidyloxypropyl) trimethoxysilane (GPS) to improve adhesion between h-B4C nanoparticles and epoxy matrix. Then, the silanized nanoparticles were added to the resin by ultrasonication and mechanical stirring techniques to produce nanocomposites. The bond structure differences of silanized B4C nanoparticles (s-B4C) and nanoparticle doped composites were investigated by using Fourier transform infrared spectroscopy. Scanning electron microscopy and energy dispersion X-ray spectroscopy (SEM-EDS) technique was used to examine the distribution of nanoparticles in the modified nanocomposites. Differential scanning calorimetry and thermogravimetric analysis techniques were used to determine the thermal properties of the neat and s-B4C doped nanocomposites. The tensile test and dynamic mechanical analysis were performed to determine the mechanical properties. When the experimental results were examined, changes in the bonding structure of the s-B4C nanoparticles doped nanocomposites and significant improvements in the mechanical and thermal properties were observed. The optimum doping ratio was determined as 2% by weight. At this doping ratio, the Tg, tensile strength and storage modulus increased approximately 18%, 35%, and 44% compared to the neat composite, respectively.  相似文献   
6.
Isocyanate-based graphene oxide-containing polyimide foams were synthesized by a semi-prepolymer method. In this method, while the first solution containing pre-polymer was derived from pyromellitic dianhydride and excess polymethylene polyphenylene isocyanate (PM200), the second solution contains dianhydride derivatives, water, catalysts, surfactants, and graphene oxide. PIFs were prepared with 0%, 0.25%, 0.50%, 0.75%, and 1% graphene oxide by weight, respectively. PIFs exhibited a minimum side reaction and urea generation was not seen for all PIFs instead of imide bonding. The addition of graphene oxide (GO) leads to a more close-packed structure. Therefore, crosslinking density and thermal stability of graphene oxide-containing polyimide foams increased. Upon the addition of 1% GO, almost seven times higher compression strength was obtained compared to neat PIFs. Also, LOI values supported the theory that thermally stable and flame retardant PIFs can be synthesized via the isocyanate-based process with GO.  相似文献   
7.
TRPM7 plays an important role in cellular Ca2+, Zn2+ and Mg2+ homeostasis. TRPM7 channels are abundantly expressed in ameloblasts and, in the absence of TRPM7, dental enamel is hypomineralized. The potential role of TRPM7 channels in Ca2+ transport during amelogenesis was investigated in the HAT-7 rat ameloblast cell line. The cells showed strong TRPM7 mRNA and protein expression. Characteristic TRPM7 transmembrane currents were observed, which increased in the absence of intracellular Mg2+ ([Mg2+]i), were reduced by elevated [Mg2+]i, and were inhibited by the TRPM7 inhibitors NS8593 and FTY720. Mibefradil evoked similar currents, which were suppressed by elevated [Mg2+]i, reducing extracellular pH stimulated transmembrane currents, which were inhibited by FTY720. Naltriben and mibefradil both evoked Ca2+ influx, which was further enhanced by the acidic intracellular conditions. The SOCE inhibitor BTP2 blocked Ca2+ entry induced by naltriben but not by mibefradil. Thus, in HAT-7 cells, TRPM7 may serves both as a potential modulator of Orai-dependent Ca2+ uptake and as an independent Ca2+ entry pathway sensitive to pH. Therefore, TRPM7 may contribute directly to transepithelial Ca2+ transport in amelogenesis.  相似文献   
8.
Investigations on the production and development of nanoparticle-reinforced polymer materials have been attracted attention by researchers. Various nanoparticles have been used to improve the mechanical, chemical, thermal, and physical properties of polymer matrix composites. Boron compounds come to the fore to improve the mechanical and thermal properties of polymers. In this study, mechanical, thermal, and structural properties of structural adhesive have been examined by adding nano hexagonal boron nitride (h-BN) to epoxy matrix at different percentages (0.5, 1, 2, 3, 4, and 5%). For this purpose, nano h-BN particles were functionalized with 3-aminopropyltriethoxysilane (APTES) to disperse the h-BN nanoparticles homogeneously in epoxy matrix and to form a strong bond at the matrix interface. Two-component structural epoxy adhesive was modified by using functionalized h-BN nanoparticles. The structural and thermal properties of the modified adhesives were investigated by scanning electron microscopy and energy dispersion X-ray spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and thermogravimetric analysis techniques. Tensile test and dynamic mechanical analysis were performed to determine the mechanical properties of the adhesives. When the results obtained from analysis were examined, it was seen that the nano h-BN particles functionalized with APTES were homogeneously dispersed in the epoxy matrix and formed a strong bond. In addition that, it was concluded from the experimental results that the thermal and mechanical properties of adhesives were improved by adding functionalized nano h-BN particles into epoxy at different ratios.  相似文献   
9.
The study aims to evaluate the technological properties of autochthonous strains (Lactobacillus sakei S15, Lactobacillus plantarum S24, L. plantarum S91, Pediococcus pentosaceus S128b and Staphylococcus carnosus G109) in Turkish dry fermented sausage (sucuk). After 24 h of fermentaPtion, all lactic acid bacteria strains reduced the pH to below 5.0, while the pH in the control group was above 5.3. The number of lactic acid bacteria strains reached 108–109 cfu g−1 during fermentation. Staphylococcus carnosus G109 remained at the inoculation level of 106 cfu g−1 during ripening. Lactobacillus sakei S15 as mono-culture showed higher TBARS values compared to other strains. The control group had the lowest L* value and autochthonous strains caused no significant difference for a* value. According to principal component analysis results, most volatile compounds were positively correlated with the group containing only L. sakei S15.  相似文献   
10.
Journal of Network and Systems Management - IoT applications have become a pillar for enhancing the quality of life. However, the increasing amount of data generated by IoT devices places pressure...  相似文献   
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