Identification of Novel Fragments Binding to the PDZ1-2 Domain of PSD-95

Inhibition of PSD-95 has emerged as a promising strategy for the treatment of ischemic stroke, as shown with peptide-based compounds that target the PDZ domains of PSD-95. In contrast, developing potent and drug-like small molecules against the PSD-95 PDZ domains has so far been unsuccessful. Here, we explore the druggability of the PSD-95 PDZ1-2 domain and use fragment screening to investigate if this protein is prone to binding small molecules. We screened 2500 fragments by fluorescence polarization (FP) and validated the hits by surface plasmon resonance (SPR), including an inhibition counter-test, and found four promising fragments. Three ligand efficient fragments were shown by ¹H,¹⁵N HSQC NMR to bind in the small hydrophobic P⁰ pockets of PDZ1-2, and one of them underwent structure-activity relationship (SAR) studies. Overall, we demonstrate that fragment screening can successfully be applied to PDZ1-2 of PSD-95 and disclose novel fragments that can serve as starting points for optimization towards small-molecule PDZ domain inhibitors.     

Effect of phosphogypsum on saline-alkalinity and aggregate stability of bauxite residue

A column experiment was conducted to investigate the effect of phosphogypsum (PG) on the saline- alkalinity, and aggregate stability of bauxite residue. Results showed that: with increasing leaching time, the concentrations of saline-alkali ions decreased while the concentration increased in bauxite residue leachate; compared with CK (control group) treatment, pH, electric conductivity (EC), exchangeable sodium percentage (ESP), sodium absorption ratio (SAR), and exchangeable Na⁺ content of bauxite residue were reduced following PG treatment; average particle sizes in aggregates following CK and PG treatments were determined to be 155 and 193 nm, respectively. SR-μCT test results also confirmed that bauxite residue following PG treatment acquired larger aggregates and larger pore diameter. These results indicate that the PG treatment could significantly modulate the saline-alkalinity, and simultaneously enhance aggregate stability of bauxite residue, which provides a facile approach to reclaim bauxite residue disposal areas.     

M2M energy saving strategy in 5G millimeter wave system

Telecommunication Systems - Machine to Machine technology has a broad application prospect in the 5G network, but there is a bottleneck in the energy consumption of intelligent devices powered by...     

土壤中有机污染物的检测技术研究进展

土壤污染防治法的实施促进了国内土壤监测业务的发展.对比分析了目前土壤中有机污染物的采样、前处理技术.挥发性有机污染物(VOCs)对采样环节的要求较高,需使用采样器和保存剂来减少挥发损失,进样前提取过程宜选用吹扫捕集等具有封闭系统的高效自动化方式.半挥发性有机污染物(SVOCs)的回收率主要受萃取、净化方式的影响,二氯甲烷和加速溶剂萃取的组合方式既快速又节约溶剂;净化材料宜选择弗罗里硅土、氧化铝类物质.选择合适的采样、前处理方法才能保证回收率、质量控制的要求.     

50型螺旋式钢板仓卷边设备理论分析与试验

结合已有卷边设备的生产工艺和特点,研发了国内首台50型螺旋式钢板仓卷边设备,并完成了4次样机调试试验.分析了新型卷边设备关键机构的工作原理,对下轧辊调节机构进行了力学计算分析,完成了卷边孔型设计.利用显示动力学软件数值模拟了5 mm钢板的冷弯成形(卷边)过程,分析了成形过程中的等效应力和等效塑性应变.通过4次样机调试试验,将调试结果与模拟结果对比.结果 表明,折弯5 mm钢板比折弯3 mm的钢板力载荷大很多,有必要研发新型的卷边设备;卷边设备的后3个工位的应力峰值比前3个工位大,其中工位6应力峰值最大;文中的卷边孔型设计合理;卷边过程的模拟结果与试验结果一致.     

Effect of nitriding atmosphere on the morphology of AlN nanofibers from solution blow spinning

High purity AlN fiber is a promising thermal conductive material. In this work, AlN fibers were prepared using solution blow spinning followed by nitridation under N₂ or NH₃ atmosphere. Soluble polymer, such as polyaluminoxane, and allyl-functional novolac resin were adopted as raw materials to form homogeneous distribution of Al₂O₃ and C nanoparticles within the fibers, which could inhibit the growth of alumina crystal and promote their nitridation process. The effect of nitriding atmosphere on the fiber morphology was investigated. XRD results showed that complete nitridation was achieved at 1300 °C in the NH₃ or at 1500 °C in the N₂ atmosphere. Hollowed fiber structure was observed when fiber was nitrided in N₂ at high temperature, which was caused by gaseous Al gas diffusion, and this phenomenon was eliminated in NH₃ atmosphere. The nitridation mechanisms in different atmosphere were analyzed in detail. It was demonstrated that the nitridation of Al₂O₃ fibers in the NH₃ atmosphere offered the favored AlN morphology and chemical quality. Flexible AlN fiber with O content of 0.7 wt% was achieved after nitriding in NH₃ at 1400 °C. The high quality AlN can be used in thermal conductive composite materials.     

某铁矿强磁尾矿反浮选回收试验研究

针对我国西部某铁矿强磁选尾矿进行了反浮选回收铁资源的试验研究, 探讨了pH值、抑制剂可溶性淀粉用量、阳离子捕收剂十二胺用量对浮选指标的影响。结果表明, 在矿浆pH=10、可溶性淀粉用量2 400 g/t、十二胺用量400 g/t条件下进行一粗一精(精选药剂用量减半)闭路反浮选, 可获得铁品位43.88%、回收率50.93%的铁精矿产品。