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.     

电网设备线夹开裂原因

某电力公司变电站用铝合金设备线夹在运行过程发生批次开裂事故,通过宏观观察、断口分析、化学成分分析、力学性能测试、冷冻模拟试验等方法,对设备线夹的开裂原因和开裂机理进行了分析。结果表明:设备线夹焊缝存在焊接缺陷,导致焊缝强度下降;设备线夹接线管底部存在积水空间,寒冷天气下积水结冰,体积膨胀,使焊缝承受设计工况外的负载而过载开裂,造成了线夹开裂。     

PVC-O管材双轴取向工艺PLC控制系统的设计

简述了PVC-O管材的生产方法.结合PVC-O管材一步加工法的生产特点,开发了PVC-O管材双轴取向工艺的PLC控制系统.阐述了该控制系统的设计方案及控制方法.     

Optical design of the Lyman alpha based beam emission spectroscopy(LAB)diagnostic on the HL-2A tokamak

In this article, we present the optical design of a novel diagnostic on the HL-2 A tokamak, i.e. the20-channel edge Lyman-alpha beam emission spectroscopy, which is a promising solution for edge density turbulence research on tokamaks, as it offers the possibility of density fluctuation measurement with a 3.3 mm spatial resolution while maintains a high temporal resolution of1 μs. The optical path, including the reflective collection optics, the high-dispersion spectrometer, and the linear detector array, is carefully optimized to obtain a good image quality and a high throughput. The maximum root mean square radius of the collection optics is 64 μm.The detected photon flux is estimated to be about 10~(11) photons/s/channel.     

一种大量元素水溶肥料的制备及其在玉米上的喷施效果

根据玉米需肥特性设计氮磷钾比例,制备了含中微量元素的大量元素水溶肥料,产品氮、磷、钾比例为2∶1∶4,属于高钾中氮低磷型.在河北省安平县前子文村和浙江省新昌县孟家塘村玉米上开展了叶面喷施试验.结果表明:玉米生物学性能得到改善,玉米产量、出籽率、百粒重与容重得到提高;与空白对照相比,平均增产率为5.45％,平均纯增收896.40元/公顷,平均产投比为5.43∶1.     

Matrix Manipulation of Directly-Synthesized PbS Quantum Dot Inks Enabled by Coordination Engineering

The direct-synthesis of conductive PbS quantum dot (QD) ink is facile, scalable, and low-cost, boosting the future commercialization of optoelectronics based on colloidal QDs. However, manipulating the QD matrix structures still is a challenge, which limits the corresponding QD solar cell performance. Here, for the first time a coordination-engineering strategy to finely adjust the matrix thickness around the QDs is presented, in which halogen salts are introduced into the reaction to convert the excessive insulating lead iodide into soluble iodoplumbate species. As a result, the obtained QD film exhibits shrunk insulating shells, leading to higher charge carrier transport and superior surface passivation compared to the control devices. A significantly improved power-conversion efficiency from 10.52% to 12.12% can be achieved after the matrix engineering. Therefore, the work shows high significance in promoting the practical application of directly synthesized PbS QD inks in large-area low-cost optoelectronic devices.     

响应面法优化白芷中欧前胡素的提取工艺

采用高效液相色谱法测定欧前胡素的含量，以水提液中欧前胡素提取率为实验指标，在单因素试验的基础之上，以提取温度、提取时间、液料比为考察因素，利用Box-Behnken Design响应面法进行三因素三水平试验设计。响应面法优选出白芷中欧前胡素的最佳提取工艺为提取温度72℃、液料比8倍、提取时间1.5 h,在该条件下欧前胡素提取率为0.97%。本研究优化的白芷中欧前胡素的提取工艺方便、稳定。     

煤矸石粉/聚酯纤维沥青混合料盐冻损伤研究EI北大核心CSCD

针对煤矸石粉替代率50%、聚酯纤维掺量0.4%的沥青混合料,开展盐冻耦合作用(NaCl溶液质量分数为0%、7.0%、13.0%、26.5%,冻融循环次数为0、2、4、6、8)下的半圆弯曲(SCB)试验,分析了盐冻耦合作用对SCB试件内部损伤劣化过程的影响.结果表明:NaCl溶液质量分数为13.0%、冻融循环为8次时,盐冻耦合作用对沥青混合料的侵蚀破坏作用最强,试件内部损伤最严重;在煤矸石粉与矿粉质量比为1∶1、聚酯纤维掺量为0.4%的条件下,沥青混合料能够形成高黏性、致密、厚实的沥青膜以及由纤维形成的三维网状结构,从而显著降低盐冻侵蚀对沥青混合料的损伤.通过Poly2D模型对SCB试件的极限拉应力损伤量进行拟合,拟合系数为0.944.     

木片筛余物高得率半化学法清洁制浆技术研究

以太阳纸业备料车间木片筛选碎料（筛余物）为原料，对其烧碱法半化学制浆的实验室工艺和生产试验进行了研究。结果表明，筛余物采用半化学法制浆可获得较高得率和环压强度的纸浆，且用碱量对纸浆性能有显著影响。相对8%NaOH （相对于绝干原料）化学预处理，采用14%NaOH化学预处理结合两段浆浓22%的高浓磨浆工艺，所制半化学浆抄造浆张的裂断长和环压指数分别达2.89 km和9.76 N·m/g，是前者的1.9倍和1.2倍，而且优于现用国内OCC废纸浆抄造浆张；生产试验得到的浆张性能指标与实验室相吻合，其中紧度和环压强度分别达到GB/T 13023—2008瓦楞芯（原）纸AA级和A级优等品要求。     

Repurposing fish waste into gelatin as a potential alternative for mammalian sources: A review

Mammalian gelatin is extensively utilized in the food industry because of its physicochemical properties. However, its usage is restricted and essentially prohibited for religious people. Fish gelatin is a promising alternative with no religious and social restrictions. The desirable properties of fish gelatin can be significantly improved by various methods, such as the addition of active compounds, enzymes, and natural crosslinking agents (e.g., plant phenolics and genipin), and nonthermal physical treatments (e.g., ionizing radiation and high pressure). The aim of this study was to explore whether the properties of fish gelatin (gel strength, melting or gelling temperature, odor, viscosity, sensory properties, film-forming ability, etc.) could be improved to make it comparable to mammalian gelatin. The structure and properties of gelatins obtained from mammalian and fish sources are summarized. Moreover, the modification methods used to ameliorate the properties of fish gelatin, including rheological (gelling temperature from 13–19°C to 23–25°C), physicochemical (gel strengths from ∼200 to 250 g), and thermal properties (melting points from ∼25 to 30°C), are comprehensively discussed. The relevant literature reviewed and the technological advancements in the industry can propel the development of fish gelatin as a potential alternative to mammalian gelatin, thereby expanding its competitive market share with increasing utility.