A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877

Loss of β-cell mass and function can lead to insufficient insulin levels and ultimately to hyperglycemia and diabetes mellitus. The mainstream treatment approach involves regulation of insulin levels; however, approaches intended to increase β-cell mass are less developed. Promoting β-cell proliferation with low-molecular-weight inhibitors of dual-specificity tyrosine-regulated kinase 1A (DYRK1A) offers the potential to treat diabetes with oral therapies by restoring β-cell mass, insulin content and glycemic control. GNF4877, a potent dual inhibitor of DYRK1A and glycogen synthase kinase 3β (GSK3β) was previously reported to induce primary human β-cell proliferation in vitro and in vivo. Herein, we describe the lead optimization that lead to the identification of GNF4877 from an aminopyrazine hit identified in a phenotypic high-throughput screening campaign measuring β-cell proliferation.     

含铌钢板坯连铸二冷目标温度及配水

讨论连铸生产过程中铸坯温度对含Nb钢高温塑性的影响，在此基础上确定铸坯在二冷段各区的表面目标温度，介绍计算二冷配水的方法，并讨论中间罐钢水温度对二冷配水的影响。     

Characterization of dynamic behavior of a spout-fluid bed with Shannon entropy analysis

Differential pressure fluctuation time series were obtained at different locations in a two-dimensional spout-fluid bed with a cross section of 300 × 30 mm and height 2000 mm. Shannon entropy analysis of differential pressure fluctuations was developed to characterize the dynamic behavior. Effects of two important operating parameters (spouting gas velocity and fluidizing gas flow rate) on the Shannon entropy were examined. It was demonstrated that a spout-fluid bed at a high spouting gas velocity or fluidizing gas flow rate was a deterministic chaos system since the Shannon entropies at all bed locations increased sharply and asymmetric unstable flows occurred. Shannon entropies were found to be significantly different at various bed locations. Shannon entropies of different flow regimes were distinct, so they were used to identify the flow regimes. The results show that the Shannon entropy helps to grasp the complex characteristics of dynamic behavior in spout-fluid beds.     

微波非接触式智能卡中射频系统和电路的设计实现

采用了Agilent公司ADS2002软件、Ansoft公司的Ensemble软件对微波非接触智能卡中射频系统和电路进行了仿真和设计。主要进行收发信道性能的仿真、天馈系统设计以及各单元电路之间匹配电路的设计。     

用RAFA方法定量解析芳烃混合物的EEM

本文介绍了降秩因子分析(RAFA)方法,它是从一个多组分混合物中直接定量计算其中某一组分,而不必知道其它组分的物种及含量的一种定量分析的数学方法。它适用于双线性的数据。本实验首先将荧光分光光度计与外接计算机相连,以获得样品的激发-发射矩阵(EEM),再用RAFA方法对蒽、萘、菲、芘、芴、(艹屈)六种标样的一至五组分的混合物进行定量分析,获得满意的结果。     

有自聚焦功能的付里叶计算全息

在制作付里叶计算全息过程中，加入适当的二次位相因子，使此种全息图在相干光照明下就可预定的位置上只再现一个像，省略了过去丙现此种计算全息图必要的付里叶透镜，并且使两个互为共轭像分离，从而拓宽了此种计算全息的应用领域，实验结果与理论分析相符。     

应用多孔阳极氧化电流—时间曲线比较壁垒膜厚

在有壁垒膜存在的表面,多孔膜的生长在氧化初期受到延迟阻碍,这一现象在直流恒压多孔阳极氧化电流一时间曲线上反映出来。电流达到稳态氧化的时间愈长,壁垒膜愈厚。文中应用此法判断了0.5MH_3BO_3介质的pH值、温度对壁垒阳极氧化膜厚的影响,并应用记录同一介质环境壁垒恒流阳极氧化的槽压一时间曲线得到验证。     

任意型一维FIR数字滤波器设计新方法

本文介绍了一种设计任意型（宽带、窄带、低阶、高阶、低通、高通、带通、带阻）一维FIR数字滤波器新方法．给出设计不同类型滤波器的统一方法。各种类型滤波器脉冲响应的设计公式简单、计算方便。该方法消除了Gibbs现象．不仅克服了优化设计中收敛速度、设计精度及初值选取等问题，而且减少设计高阶滤波器的时间。最后，本文给出了各种类型滤波器设计的仿真结果。     

热场致发射电子源曝光系统的技术现状和应用前景

高亮度、长寿命的热场致发射(Thermal field emitter)阴极自七十年代中期已受到人们的关注和重视,历经十多年在理论分析、工艺制备和实验研究上做了大量工作之后,于1988年在电子束曝光机上的应用中取得了突破性进展。用晶向为(100)的钨和具有低逸出功的锆制成的(Zr/O/W)热场致发射阴极在四千小时的使用寿命下亮度值超过六硼化镧阴极一个数量级以上,最近的实验结果表明:在工件台上小束斑下能得到接近两千安培每平方厘米的束流密度,而且四十小时内束流稳定度接近千分之一。显然,这几个表征曝光系统综合技术性能的重要指标,说明多年困扰于各种电子束曝光系统(特别是高斯圆斑电子束系统)在高分辨率情况下生产率较低的技术难题已经得到了比较圆满的解决。 八十年代末期,当热场致发射电子源曝光系统的技术关键解决后,这项技术就成为技术发达国家,特别是美国和日本,在电子束曝光领域进行技术竞争的热点;九一年五月底在美国召开的国际三束会议上有关场致发射阴极和MEBES—4型机已经采用TFE的最新报道充分证实了这项技术在电子束曝光技术应用中的重要地位和发展潜力。