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.     

功能性小麦品种的概念、类别和发展前景（网络首发、推荐阅读）

结合全球倡导的营养导向型农业和功能性食品的内容，首次提出“功能性小麦品种”的概念，将其定义为“含有对人体健康有益的活性成分，可调节人体有益代谢，能给人体健康带来某种益处或满足特定人群的特殊需求，同时可以作为日常食物的口感正常、无毒副作用的小麦品种类型”；结合疫情警示和我国进入后工业时代后，人们需求必将由“吃得饱”、“吃得好”向“吃得健康”转变，因而提出继高产品种、优质品种之后培育“功能性小麦品种”的育种目标。根据多年关于小麦淀粉、蛋白、酯类和其他成分的功能研究结果，介绍新育成的“麦黄酮”、“高色素”、“高抗性淀粉”、“富锌”、“低醇溶蛋白”和“低植酸”等功能性小麦新品种（系）的营养特性和农艺产量状况；根据“健康中国2030”规划等国家战略，进行“功能性品种培育是解决我国功能性食品‘卡脖子’的关键基础，一种功能性品种可以形成一类功能性食品，多种功能性品种可以形成我国功能性面制品产业，推动我国整个食品工业的发展”的前景展望；根据功能性品种及其食品的稳定性和可靠性是产品和市场的“生命线”，从对消费者负责的高度，提出关于“功能性农作物品种审定导向和组建功能性成分检测机构；编制有关功能性品种和食品的国家或行业标准，设立功能性食品和功能性农作物品种的商业标志，保证我国功能性农作物品种及其食品健康发展”等方面的具体建议。     

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...     

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.     

新型绿化用结构土在大型主题公园中的应用

北京某文旅主题公园项目施工中,针对临近道路承载影响植物根系发育和植物根系发育过程中对面层破坏的问题,研究新型环保绿化用结构土技术.使用碎石、粘壤土、土壤改良剂、水等材料的最佳配合比,制成了一种新型绿化用结构土,既满足了硬质路面承载要求,又满足了植物根系地下环境生长需求,还提高了海绵城市效能.     

某特钢工业厂房办公楼结构设计

特钢工业厂房办公楼由2栋长90.6 m、宽34.2 m、高36.5 m的塔楼组成,两个塔楼之间2层设置钢平台,一端铰接,一端滑移.通过方案比选,两塔楼均采用钢框架(局部设支撑)结构体系,标准轴网为8.4 m×9.0m,结构布置基本对称,相邻处端部一跨存在斜柱.针对斜柱对结构的不利影响,对结构进行了 pushover分析,并采取了相应的措施;2层的钢平台跨度较大,进而做了舒适度分析,结果表明,满足规范的要求.     

磨矿动力学研究现状及应用

磨矿动力学是描述被磨物料的磨碎速率与磨矿时间之间关系规律的一种数学模型，对分析物料在磨矿过程中的粒级及能量变化具有重要作用。为充分发挥磨矿动力学在磨矿过程中的作用，论文在分析国内外研究现状的基础上，系统介绍了两种典型的磨矿动力学模型：m阶磨矿动力学模型和磨矿总体平衡动力学模型，分析了模型中各参数的含义；以磨矿总体平衡动力学模型为重点，分析了破碎速率函数和破碎分布函数的求解方式，包括零阶产出率法、奥-勒理论简算法、卡普尔G-H算法以及经验公式法等；从物料性质、磨矿介质及配比、磨矿方式及参数、化学添加剂等几个方面分析了影响磨矿动力学模型的因素；指出了磨矿动力学模型在矿物加工工程领域的应用现状并对其未来的研究方向提出展望。研究表明磨矿动力学在矿物加工领域具有广泛而重要的应用，为进一步改善磨矿工艺提供了理论依据。     

我国水-能源-粮食耦合关系及影响因素

为缓解我国水、能源和粮食资源紧张问题，促进资源可持续利用，构建水-能源-粮食系统，利用耦合协调度模型对我国的30个省（自治区、直辖市）进行测算,并利用空间杜宾模型分析主要影响因素。结果表明：2003—2017年，我国能源、粮食评价[JP]指数高于水资源评价指数，系统综合评价指数逐年递增；大部分省份耦合协调度处于初级协调水平且呈现逐年上升的态势，个别省份耦合协调度濒临失调；耦合协调度空间自相关性较强，虽有明显波动，但是呈现逐年加强的态势；影响耦合协调度的主要因素有从业人口数、固定资产投资额、人均生产总值、人口总数、[JP]文盲人口占比、工业污染排放、城镇化。