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.     

基于常规技术的新型车身套色工艺方案

介绍了一种在不改变原有工艺路线,不需要返线或另建专用套色线就可以实现车身套色的新型工艺,其基本上不受套色车产能比例限制,具有投资少、能耗低、产能柔性程度高等特点.     

基于密闭爆发器试验的发射装药内弹道性能预估

为了预估发射装药的内弹道性能,建立了一种基于密闭爆发器试验检测发射药的静态燃烧性能参数进而预测其装药内弹道性能的方法,采用不同批次的单樟-5/7发射药进行了装药性能预估计算,并基于30 mm火炮对内弹道性能预估精度进行了试验验证。结果表明,采用所建立的基于密闭爆发器试验的发射装药内弹道性能预估方法计算获得的最大膛压为376.0 MPa,与试验测试的膛压平均值388.7 MPa的计算误差为3.27%;计算的炮口初速为1143.5 m/s,与试验测试的炮口初速平均值1156.3 m/s的计算误差为1.11%。所建立的基于密闭爆发器试验的发射装药内弹道性能预估方法具有较高的精度,可对发射药样品不同批次间的内弹道性能进行高效精确的预估,为长期贮存发射药使用寿命的判定及发射药产品的出厂校验提供了一种高效低成本的弹道性能评价方法。     

Semantic word shifts in a scientific domain

Understanding semantic word shifts in scientific domains is essential for facilitating interdisciplinary communication. Using a data set of published papers in the field of information retrieval (IR), this paper studies the semantic shifts of words in IR based on mining per-word topic distribution over time. We propose that semantic word shifts not only occur over time, but also over topics. The shifts are examined from two perspectives, the topic-level and the context-level. According to the over-time word-topic distribution, stable words and unstable words are recognized. The diverging and converging trends in the unstable type reveal characteristics of the topic evolution process. The context-level shifts are further detected by similarities between word vectors. Our work associates semantic word shifts with the evolving of topics, which facilitates a better understanding of semantic word shifts from both topics and contexts.     

矿用无人卡车国内外研究现状及关键技术

分析了国内外露天矿山用卡车无人驾驶技术发展现状,详细介绍了露天矿山卡车无人驾驶关键技术;通过分析对比前装线控和后装线控两种技术路线的优缺点以及超声波雷达、毫米波雷达、激光雷达、4D光场智能感知系统、红外传感器、视觉传感器等环境感知技术的优缺点;提出多传感器高度融合将是露天矿山卡车实现全天候环境感知的发展方向。通过分析对比惯性导航系统、GNSS差分定位技术、车联网定位技术、电子地图定位技术、视觉传感器等定位导航技术的差异,指出多定位技术融合是露天矿山无人驾驶卡车定位方式的必然选择。结合露天煤矿的生产实际,提出将现有的无人驾驶各种技术算法与露天矿山标准作业流程有机融合是实现卡车无人驾驶的必由之路。最后指出无人驾驶卡车应用5G技术是露天矿山安全生产的关键和核心,是无人驾驶的必备技术。     

Nb和时效时间对热轧中锰TRIP钢中P偏聚的影响

热轧态中锰TRIP钢首先经650 ℃退火2 h,随后在550 ℃进行等温时效热处理,采用场发射扫描电镜(FE-SEM)研究该钢中P的偏聚和时效析出行为的变化情况。结果表明,中锰TRIP钢中P在晶界的偏聚是一种非平衡偏聚现象,临界时间约为50 h,与理论计算结果48 h较为吻合。在局部偏聚区域内,C与P存在共偏聚的关系,即P偏聚量高的地方,C含量也高。而合金元素Nb具有抑制P偏聚的效果,在20~70 h时效时间内,可以相对降低6.57%~19.5%的最大P偏聚量。根据电子背散射衍射(EBSD)菊池线分析,P偏聚量低于2.28at%时,P为固溶状态,高于2.28at.%时,P为析出状态。     

A Review on Friction Stir Processing of Titanium Alloy: Characterization,Method, Microstructure,Properties

Metallurgical and Materials Transactions B - In the past two decades, friction stir processing (FSP) technology has received considerable attention. FSP can be used to adjust and control the...