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51.
Dr. Thomas Le Bihan Dr. Cathryn H. S. Driver Dr. Thomas Ebenhan Dr. Nathalie Le Bris Dr. Jan Rijn Zeevaart Prof. Dr. Raphaël Tripier 《ChemMedChem》2021,16(5):809-821
An improved glucose-chelator-albumin bioconjugate (GluCAB) derivative, GluCAB-2Mal, has been synthesized and studied for in vivo 64Cu-PET/CT imaging in breast cancer mice models together with its first-generation analogue GluCAB-1Mal. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [64Cu]Cu-GluCAB-2Mal (99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [64Cu]Cu-GluCAB-2Mal and previous-generation [64Cu]Cu-GluCAB-1Mal encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [64Cu]Cu-GluCAB-2Mal was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [64Cu]Cu-Glu-CAB-2Mal. 相似文献
52.
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
53.
In this study, chemically bonded phosphate ceramic coatings (CBPCCs) with different contents of aluminum phosphate (AP) are prepared on stainless steel (AISI 304L). Differential scanning calorimetry, X-ray diffraction, contact angle test, and a tribocorrosion experiment are carried out to clarify the role of AP in the tribocorrosion performance of CBPCCs. The results show that, with the increase in the AP content, the enthalpy of curing increases because of the greater formation of the bonding phase AlPO4. Both in static corrosion and in tribocorrosion, the corrosion current density of CBPCCs achieves the lowest value when the weight ratio of AP to polytetrafluoroethylene is about 0.78. Additionally, the influence mechanism of AP on tribocorrosion is clarified. AlPO4 from the reaction between AP and Al2O3 has excellent mechanical properties and can enhance the wear resistance of CBPCCs by reducing the mechanical wear and the increased wear due to corrosion. The alumina particles wrapped by AlPO4 can form a dense and smooth surface and change the direction of electrolyte propagation, which leads to the increase in the tribocorrosion resistance of CBPCCs. 相似文献
54.
Zhongchao Fu Xiaodong Li Mu Zhang Qi Zhu Ji-Guang Li Jiao He Xing'an Wang Xudong Sun 《Journal of the American Ceramic Society》2021,104(6):2689-2701
An easy albeit quite effective deionization suspension treatment was adopted to alleviate the detrimental effects related to the hydrolysis of Y2O3 in an aqueous medium. Fabrication of highly transparent Y2O3 ceramics with a fine grain size via air pre-sintering and post–hot isostatic pressing (HIP) treatment without using any sintering additive was achieved using the treated suspensions. The hydrolysis issue of Y2O3 powder in an aqueous medium was effectively alleviated by using deionization treatment, and a well-dispersed suspension with a low concentration of dissolved Y3+ species was obtained. The dispersed suspensions were consolidated by the centrifugal casting method, and the green bodies derived from the suspension of 35.0 vol% solid loading showed an improved homogeneity with a relative density of 52.1%. Fully dense Y2O3 transparent ceramic with high transparency was obtained by pre-sintering consolidated green compacts at a low temperature of 1400°C for 16 h in air followed by a post-HIP treatment at 1550°C for 2 h under 200 MPa pressure. The sample had a fine average grain size of 690 nm. The in-line transmittance of the sample reached 83.3% and 81.8% at 1100 nm and 800 nm, respectively, very close to the theoretical values of Y2O3. 相似文献
55.
Seplyarskii B. S. Kochetkov R. A. Lisina T. G. Abzalov N. I. 《Combustion, Explosion, and Shock Waves》2021,57(3):334-342
Combustion, Explosion, and Shock Waves - This paper touches upon the effect of a polyvinyl butyral content (0–2.3%) on the combustion of a Ti + C granular... 相似文献
56.
Claudia Paredes Francisco J. Martínez-Vázquez Hamada Elsayed Paolo Colombo Antonia Pajares Pedro Miranda 《Journal of the European Ceramic Society》2021,41(1):892-900
Bioactive ceramic scaffolds for bone regeneration consisting of a three-dimensional mesh of interpenetrating struts with square section were fabricated via Digital Light Processing (DLP). The ability of the technique to manufacture 3D porous structures from β-tricalcium phosphate (β-TCP) powders with different dimensions of struts and pores was evaluated, identifying the possibilities and limitations of the manufacturing process. Small pore sizes were found to seriously complicate the elimination of excess slurry from the scaffold’s innermost pores. The effect of the strut/pore size on the mechanical performance of the scaffolds under compressive stresses was also evaluated, but no significant influence was found. Under compressive stresses, the structures resulted weaker when tested perpendicularly to the printing plane due to interlayer shear failure. Interlayer superficial grooves are proposed as potential failure-controlling defects, which could also explain the lack of a Weibull size effect on the mechanical strength of the fabricated DLP scaffolds. 相似文献
57.
Han Chen Shunzo Shimai Jin Zhao Xiaojian Mao Jian Zhang Guohong Zhou Shiwei Wang 《Journal of the European Ceramic Society》2021,41(6):3838-3843
Alumina platelets were arranged horizontally in submicron alumina particles by shear force in the flow of slurries during casting. The obtained alumina green bodies with platelets were pressureless-sintered in vacuum, producing ceramics with thoroughly oriented grains and high transmittance. The effects of sintering parameters on the densification, microstructure evolution, and orientation degree of alumina ceramics were investigated and discussed. The results showed that the densification, grain size, orientation degree, and in-line transmittance were increased with increasing sintering temperature. The enhancement of orientation degree was mainly coherent with grain growth. The grain-oriented samples exhibited a much higher in-line transmittance (at 600 nm) of 61 % than that of the grain random sample (29 %). Moreover, the transmission remained a high level in the ultraviolet range (<300 nm). 相似文献
58.
Kyle L. Covington Alexander K. Goroncy Teresa E. Lehmann Zuhao Kou Heng Wang Vladimir Alvarado 《American Institute of Chemical Engineers》2021,67(2):e17074
Microtomography (μCT) and nuclear magnetic resonance (NMR) have been used to characterize porous media for decades. Magnetic resonance imaging (MRI) enables direct visualization of pore architecture and many pulse sequences exist. In this work, we tested the MRI pulse sequence Zero Echo Time (ZTE) to study sandstone and carbonate for its ability to address short relaxation times. We aimed at resolving two fluid conduit scales, that is, pores and fractures. In this research, we study tighter porous systems than those previously reported using ZTE. Additionally, pore cluster analysis (PCA), combined with ZTE, can be used to analyze pore-fracture connectivity of relatively large core plugs. We show that ZTE can resolve two-scale pore systems simultaneously, that is, fractures and pores. By combining time-domain NMR pore-size analysis and PCA, we show that careful selection of resolution is necessary to understand transport in porous media. 相似文献
59.
Lalitha Kodumudi Venkataraman Tingting Zhu Monica Pinto Salazar Kathrin Hofmann Aamir Iqbal Waidha J. C. Jaud Pedro B. Groszewicz Jürgen Rödel 《Journal of the American Ceramic Society》2021,104(5):2201-2212
Na1/2Bi1/2TiO3-based materials have been earmarked for one of the first large-volume applications of lead-free piezoceramics in high-power ultrasonics. Zn2+-doping is demonstrated as a viable route to enhance the thermal depolarization temperature and electromechanically harden (1-y)Na1/2Bi1/2TiO3-yBaTiO3 (NBT100yBT) with a maximum achievable operating temperature of 150 °C and mechanical quality factor of 627 for 1 mole % Zn2+-doped NBT6BT. Although quenching from sintering temperatures has been recently touted to enhance TF-R, with quenching the doped compositions featuring an additional increase in TF-R by 17 °C, it exhibits negligible effect on the electromechanical properties. The effect is rationalized considering the missing influence on conductivity and therefore, negligible changes in the defect chemistry upon quenching. High-resolution diffraction indicates that Zn2+-doped samples favor the tetragonal phase with enhanced lattice distortion, further corroborated by 23Na Nuclear Magnetic Resonance investigations. 相似文献
60.