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21.
Viktoria M. S. Kjær Loukas Ieremias Dr. Viktorija Daugvilaite Dr. Michael Lückmann Prof. Thomas M. Frimurer Prof. Trond Ulven Prof. Mette M. Rosenkilde Dr. Jon Våbenø 《ChemMedChem》2021,16(17):2623-2627
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
22.
William M. Pitts Martin Werrel Marco Fernandez Mary A. Long Evan A. Eisenberg James Filliben Cory D. Runyon 《火与材料》2021,45(1):127-154
Fire spread and growth on real‐scale four cushion mock‐ups of residential upholstered furniture (RUF) were investigated with the goal of identifying whether changes in five classes of materials (barrier, flexible polyurethane foam, polyester fiber wrap, upholstery fabric, and sewing thread), referred to as factors, resulted in statistically significant changes in burning behavior. A fractional factorial experimental design plus practical considerations yielded a test matrix with 20 material combinations. Experiments were repeated a minimum of two times. Measurements included fire spread rates derived from video recordings and heat release rates (HRRs). A total of 13 experimental parameters (3 based on the videos and 10 on the HRR results), referred to as responses, characterized the measurements. Statistical analyses based on Main Effects Plots (main effects) and Block Plots (main effects and factor interactions) were used. The results showed that three of the factors resulted in statistically significant effects on varying numbers of the 13 responses. The Barrier and Fabric factors had the strongest main effects with roughly comparable magnitudes. Foam was statistically significant for fewer of the responses and its overall strength was weaker than for Barrier and Fabric. No statistically significant main effects were identified for Wrap or Thread. Multiple two‐term interactions between factors were identified as being statistically significant. The Barrier*Fabric interaction resulted in the highest number of and strongest statistically significant effects. The existence of two‐term interactions means that it will be necessary to consider their effects in approaches designed to predict the burning behavior of RUF. 相似文献
23.
Olga Yu Kurapova Sergey M. Shugurov Evgenia A. Vasil'eva Daniil A. Savelev Vladimir G. Konakov Sergey I. Lopatin 《Ceramics International》2021,47(8):11072-11079
Ceria-based solid solutions are important materials for high- and medium-temperature electrochemical applications. However, the stabilities of both binary and ternary ceria-based solid solutions are insufficient at elevated temperatures, which limits their application as solid electrolytes or SOFC cathodes. Data on the high-temperature stability of ceria-based ceramics are unavailable in the literature. In the present study, we report a thermodynamic stability investigation of Y2O3-CeO2 and Y2O3-ZrO2-CeO2 solid solutions. The thermal prehistories of binary and ternary systems were investigated using STA, XRD, and ESCA techniques. The vaporization processes were investigated in the temperature range of 1577–2227°С via the Knudsen effusion mass spectrometry technique. Using data on the component activity in solid-phase thermodynamic properties of Y2O3-CeO2 solid solutions, which is represented as the Gibbs energy, the excess Gibbs energy was calculated as a function of the ceria mol. %. It was shown that the reduction of Ce4+ to Ce3+ in Y2O3-CeO2 and Y2O3-ZrO2-CeO2 solid solutions corresponds to less-negative Gibbs energy compared to ZrO2-CeO2 solid solutions. 相似文献
24.
Journal of Signal Processing Systems - Convolutional Neural Networks (CNNs) have improved several computer vision applications, like object detection and classification, when compared to other... 相似文献
25.
We considered the magnetohydrodynamic (MHD) free convective flow of an incompressible electrically conducting viscous fluid past an infinite vertical permeable porous plate with a uniform transverse magnetic field, heat source and chemical reaction in a rotating frame taking Hall current effects into account. The momentum equations for the fluid flow during absorbent medium are controlled by the Brinkman model. Through the undisturbed state, both the plate and fluid are in a rigid body rotation by the uniform angular velocity perpendicular to an infinite vertical plate. The perpendicular surface is subject to the homogeneous invariable suction at a right angle to it and the heat on the surface varies about a non-zero unvarying average whereas the warmth of complimentary flow is invariable. The systematic solutions of the velocity, temperature, and concentration distributions are acquired systematically by utilizing the perturbation method. The velocity expressions consist of steady-state and fluctuating situations. It is revealed that the steady part of the velocity field has a three-layer characteristic while the oscillatory part of the fluid field exhibits a multi-layer characteristic. The influence of various governing flow parameters on the velocity, temperature, and concentration are analyzed graphically. We also discuss computational results for the skin friction, Nusselt number, and Sherwood number in the tabular forms. 相似文献
26.
Castro Mateus B. Souza Raphael R. N. Junior Agord M. P. Lima Eduardo R. Manera Leandro T. 《Analog Integrated Circuits and Signal Processing》2021,109(3):647-656
Analog Integrated Circuits and Signal Processing - This paper presents the complete design of a phase locked loop-based clock synthesizer for reconfigurable analog-to-digital converters. The... 相似文献
27.
Krzysztof M. Tokarz Wojciech Wesoowski Barbara Tokarz Wojciech Makowski Anna Wysocka Roman J. Jdrzejczyk Karolina Chrabaszcz Kamilla Malek Anna Kostecka-Gugaa 《International journal of molecular sciences》2021,22(2)
Grass pea (Lathyrus sativus) is a leguminous plant of outstanding tolerance to abiotic stress. The aim of the presented study was to describe the mechanism of grass pea (Lathyrus sativus L.) photosynthetic apparatus acclimatisation strategies to salinity stress. The seedlings were cultivated in a hydroponic system in media containing various concentrations of NaCl (0, 50, and 100 mM), imitating none, moderate, and severe salinity, respectively, for three weeks. In order to characterise the function and structure of the photosynthetic apparatus, Chl a fluorescence, gas exchange measurements, proteome analysis, and Fourier-transform infrared spectroscopy (FT-IR) analysis were done inter alia. Significant differences in the response of the leaf and stem photosynthetic apparatus to severe salt stress were observed. Leaves became the place of harmful ion (Na+) accumulation, and the efficiency of their carboxylation decreased sharply. In turn, in stems, the reconstruction of the photosynthetic apparatus (antenna and photosystem complexes) activated alternative electron transport pathways, leading to effective ATP synthesis, which is required for the efficient translocation of Na+ to leaves. These changes enabled efficient stem carboxylation and made them the main source of assimilates. The observed changes indicate the high plasticity of grass pea photosynthetic apparatus, providing an effective mechanism of tolerance to salinity stress. 相似文献
28.
Abidur Rahman Makoto Kobayashi Kotaro Sugimoto Yuta Endo Manabu Kojima Shigenori Furukawa Takafumi Watanabe Shu Soeda Yuko Hashimoto Keiya Fujimori Hideki Chiba 《International journal of molecular sciences》2021,22(7)
Background: Within the claudin (CLDN) family, CLDN12 mRNA expression is altered in various types of cancer, but its clinicopathological relevance has yet to be established due to the absence of specific antibodies (Abs) with broad applications. Methods: We generated a monoclonal Ab (mAb) against human/mouse CLDN12 and verified its specificity. By performing immunohistochemical staining and semiquantification, we evaluated the relationship between CLDN12 expression and clinicopathological parameters in tissues from 138 cases of cervical cancer. Results: Western blot and immunohistochemical analyses revealed that the established mAb selectively recognized the CLDN12 protein. Twenty six of the 138 cases (18.8%) showed low CLDN12 expression, and the disease-specific survival (DSS) and recurrence-free survival rates were significantly decreased compared with those in the high CLDN12 expression group. We also demonstrated, via univariable and multivariable analyses, that the low CLDN12 expression represents a significant prognostic factor for the DSS of cervical cancer patients (HR 3.412, p = 0.002 and HR 2.615, p = 0.029, respectively). Conclusions: It can be concluded that a reduced CLDN12 expression predicts a poor outcome for cervical cancer. The novel anti-CLDN12 mAb could be a valuable tool to evaluate the biological relevance of the CLDN12 expression in diverse cancer types and other diseases. 相似文献
29.
Glass and Ceramics - An analysis of the specific mechanisms of the influence of the state of the grain structure on the thermoelectric properties (electrical resistivity and total thermal... 相似文献
30.
N.A. Zhuk M.G. Krzhizhanovskaya N.A. Sekushin V.V. Kharton B.A. Makeev V.A. Belyy R.I. Korolev 《Ceramics International》2021,47(14):19424-19433
The solid solutions based on the pyrochlore-type system Bi2MgNb2-xTaxO9 were formed in the compositional range х = 0–2.0 (Bi1·6Mg0·8Nb1.6-tTatO7.2, t = 0–1.6). The Rietveld method was used to refine the structure for Bi2MgNb2-xTaxO9 (x = 0, 1.0, 2.0). The increasing tantalum content led to the slight decrease in the cubic unit cell parameters from 10.56934 (4) Å for x = 0 and 10.54607 (3) Å for x = 2 (sp.gr. Fd-3m:2). At the same time, tantalum additions suppressed grain growth in the pyrochlore ceramics during sintering and made it possible to obtain materials with an average grain size of 1–2 μm (Bi1·6Mg0·8Ta1·6O7.2). The increase in the Ta5+ concentration led to the decrease in the dielectric permeability from 104 (Bi1·6Mg0·8Nb1·6O7.2) to 20 (Bi1·6Mg0·8Ta1·6O7.2) at room temperature, while the dielectric loss tangent remained lower than 0.002, which is due to the small grain size and the high porosity of the samples. An increase in temperature has practically no effect on the values of the dielectric permittivity in the entire frequency range. The samples have weak through conductivity. The activation energies of electrical conductivity varied in the range of 0.84–1.00 eV, and the less tantalum, the lower the activation energy. The electrical properties of the samples at 200 Hz to 1 MHz are described by the simplest parallel scheme. 相似文献