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.     

Smart firefighting construction in China: Status,problems, and reflections

“Smart firefighting” construction as a part of the “smart city” has been a concern of the public security and fire agencies at all levels. In this study, the status, problems, and reflections of “smart firefighting” construction in China are discussed. A recent survey indicates that China has launched its smart firefighting construction and initially created a new perspective on its regional smart firefighting work based on three main aspects: intelligent disaster perception by Internet of Things (IoT) construction, intelligent disaster prevention by big data construction, and intelligent disaster disposal by emergency rescue platform construction. However, the current smart firefighting construction in China still has some prominent problems such as the data interconnectivity and normalized management of various platforms, the extensibility of smart firefighting platforms, and the intelligent level of smart firefighting researches, which need to be solved urgently. Therefore, we argue that smart firefighting construction in China should establish data interconnectivity, industrial normalized management, 2D/3D geographic information interaction and extension, high-integration fire protection theory, and many other aspects in the near future and truly realize firefighting visualization and efficient data applications for 4D time space. This study could provide valuable reference for smart firefighting and smart city construction.     

Decoder side information generation techniques in Wyner-Ziv video coding: a review

Multimedia Tools and Applications - In Wyner-Ziv (WZ) video coding, decoder side information (SI) takes a key role in a WZ video codec among other building blocks. In this paper, we review the...     

制备金属铪的新进展

金属铪在核能、航天以及军工领域有着得天独厚的优势,国内外对于金属铪的研究正如火如荼的进行。锆铪相伴而生,本文介绍了锆铪的火法和湿法分离,综述了金属热还原法和熔盐电脱氧法制备金属铪通过熔盐电解法、碘化精练法、电子束熔炼法精炼金属铪,就各种方法的优缺点和绿色生产的需求来看,新型熔盐电脱氧法和联合精炼法是值得发展和探究的方向。     

液压支架立柱拆装机构设计

拆柱机由电动机匹配乳化液泵将电能转化为泵的液压能,带动液压马达回转作为拆装柱的动力。     

Q690钢焊接接头微观组织对冷裂纹的影响研究

分析了Q690钢手工电弧焊与气体保护焊焊接冷裂纹产生与微观组织的联系。结果表明: 焊接冷裂纹起源于斜Y坡口根部, 沿熔合区、焊缝扩展至焊缝表面;2种工艺焊接的接头组织硬度均较母材高, 而塑性较差。热影响区为马氏体、贝氏体与铁素体混合组织, 焊缝组织由先共析铁素体、侧板条铁素体、贝氏体和针状铁素体等组成, 针状铁素体抗裂纹扩展能力较其他组织强。在2种焊接方法对应断口中观察到了冷裂纹起裂、扩展与断裂区的不同形貌, 起裂与扩展区存在塑性变形, 而断裂区为解理断裂。     

基于DoG检测图像特征点的快速二进制描述子

针对SIFT描述子实时性差和传统二进制描述子对尺度、旋转和视角变化鲁棒性差的问题,本文通过优化采样模式和添加灰度差分不变量比较测试进行改进,提出了一种鲁棒性更高的二进制描述子。首先,设计了一种尺度关联、编号标记的采样模式;然后,旋转采样模式中各采样点到特定位置,确保描述子尺度、旋转不变性;接着,分析了采样点点对模式对描述子的影响,选择使用机器学习训练后的128对采样点对;最后,选择灰度值比较测试及梯度绝对值和比较测试构建二进制描述子。实验中采用DoG检测图像关键点,结果表明:本文提出的描述子在描述子构建和描述子匹配上比SIFT描述子分别快84%和67%;在有视角变化的图像匹配上,准确率比传统的二进制描述子高3%~5%,召回率平均要高30%以上。本文提出的特征点描述方法适用于时间要求高的图像匹配领域。     

吐哈盆地克尔碱凹陷煤层煤质特征与成煤环境

为了揭示吐哈盆地克尔碱凹陷不同矿区煤质形成条件，探讨该区煤质与成煤环境的关系，基于对主采煤层样品工业分析、有害组分及灰成分指标等数据分析，在对克尔碱凹陷地层分布、含煤岩系特征等基本地质条件分析的基础上，运用煤地质学、煤岩学、煤化学等理论和方法，系统总结凹陷内各矿区煤层赋存特征、煤质特征，探讨区内煤岩煤质与成煤环境的关系。结果表明：研究区自西向东划分6个主要矿区,区内煤层主要发育于中侏罗统西山窑组（J2x）和下侏罗统八道湾组（J1b）地层之中。研究区煤质呈低灰、低硫、高挥发分特征，煤灰成分以SiO2、Al2O3为主。综合分析表明，研究区中-下侏罗统主要煤层形成于湖泊-河流三角洲淡水沉积环境，具陆相成煤特征，成煤环境温暖潮湿。     

酸性废水中As(Ⅲ)、Cu(Ⅱ)与铁粉的反应行为

在Fe-As(Ⅲ)-Cu(Ⅱ)-H₂O体系中, 研究了酸性废水中As(Ⅲ)、Cu(Ⅱ)与金属铁粉的反应行为, 考察了反应过程中As在气、液、固三相中的分配比。结果表明, As(Ⅲ)和Cu(Ⅱ)离子被Fe还原为单质As和Cu后, As、Cu进一步结合成Cu₅As₂等金属间化合物, 从而促进As(Ⅲ)沉淀反应的发生, 且无AsH3生成。在反应时间40min、铁粉过量系数1.2、溶液初始pH=0.0、温度40 ℃、Cu/As摩尔比1.0条件下, As在气、液、固三相中的分配比分别为0、20.7%和79.3%, 沉砷率为79.3%。