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.     

豫西雷门沟钼矿水文地质条件分析及涌水量预测

豫西熊耳山雷门沟钼矿床位于东秦岭多金属成矿带东段,是已探明的超大型斑岩型钼矿,前人研究程度高、地质成果丰硕,但对矿床开采技术条件方面研究较少。本次通过地质调查工程、水文地质试验等方法,从水文地质角度,对雷门沟钼矿床水文地质条件进行研究,填补了该方面的空白,丰富了研究成果；采用水文地质比拟法预测未来矿坑最大排水量2613 m³/d,经实践检验结果较为可靠；总结的采坑排水量预测方法、含水层特点、矿床充水因素以及防治水措施,以期对该区域水文地质工作具有参考价值。     

Research on the identification performance of UHF RFID system considering the correlation of cascaded channel

The identification rate of UHF RFID system was restricted by multipath propagation effects.The system identification performance was studied considering the correlation coefficient between forward and reverse channels.Based on the generalized Rician fading channel model,the analytical expression of identification rate was derived under independent,full correlation and correlation cases.Compared with the existing analysis,the proposed uniform calculation formula of identification rate was for any correlation coefficient and kinds of channel conditions.The numerical computation and Monte-carlo simulations show that the influences of different correlation coefficients,channel conditions,sensitivity and distance on the identification rate.     

智能化救援监控系统在煤矿安全生产中的应用

针对煤矿发生事故后传统救援监控系统无法实时对井下人员进行动态定位，导致矿井救援盲目性大、救援效率差、救援难度大等技术难题，为了进一步提高煤矿救援效率，通过技术研究，设计了一套以通信基站为核心的智能化救援监控系统，分析了该系统结构组成、工作原理，通过在担水沟煤矿井下实际应用效果来看，智能化救援监控系统对人员定位精准度达95%，实现人员动态位置三维成像，救援效率提高至80%以上，有效缩短了煤矿事故救援时间，取得了显著应用成效。     

室内机组的开发与应用

随着市场的发展,精品超市和改造店铺逐渐增多,需要一种更加适合的制冷机组来满足市场的需求。本文提供了一种新型的解决方案,解决了现有机组存在的高噪音和高成本问题,不仅提高了制冷效率,而且节约能源,保护环境。     

黄浦江下游吴淞口站低潮位重现期研究

黄浦江为感潮河流,低潮位重现期的确定对黄浦江航道的设计具有重要意义。为了准确估计黄浦江低潮位的重现期,以黄浦江下游吴淞口站年最低潮位序列为例,在对样本进行三性审查的基础上,分别采用传统的数理统计方法和时变矩方法进行水文频率分析。结果表明:吴淞口站年最低潮位序列在1996年发生了变异;还现修正后的序列服从位置参数线性时变的GEV模型,低潮位存在缓慢的上升趋势;一致性条件下百年一遇低潮位约为0.261 m,在非一致性条件下其重现期增大为150 a。非一致性条件下的重现期增大说明黄浦江现有的航道设计标准偏安全,航道通航保证率提高。     

Modeling Impact of ROADM Intra-Node Add/Drop Contention on a Single Node Lightpath Blocking Performance

We propose an analytical model to evaluate the lightpath blocking performance for a single ROADM node with intra-node add/drop contention,in which the number of lightpaths that can be added/dropped with the same wavelength is limited by the add/drop contention factor.Different models of traffic load per nodal degree are considered to validate the effectiveness of the analytical model.The simulation results show that the proposed analytical model is effective in predicting the performance for different values of add/drop contention factor C and for variable offered loads at the node.The add/drop contention factor shows an important impact on the lightpath blocking performance and properly raising the contention factor can significantly improve the lightpath blocking performance.When the add/drop contention factor C exceeds a certain level,the performance of a ROADM with intra-node contention is close to that of a contentionless ROADM.     

Preparation and Properties of a New Mediumdensity and High-strength Ceramic Proppant

Based on the needs of the market,a new 52 MPa medium-density and high-strength ceramic proppant was prepared by adopting third grade bauxite and clay as raw materials and using the solid phase sintering method,and the effect of the firing temperature on the microstructure,phase composition and mechanical properties of the ceramic proppant was studied. The broken resistance mechanism of this ceramic proppant was also discussed. The results show that the main phases of the prepared ceramic proppant are mullite and corundum; the broken rates are 3. 92% and 7. 21% under 52 MPa and69 MPa,respectively.     

Experimental and numerical study on compressive performance of perforated brick masonry after fire exposure

This paper discusses the compressive performance of perforated brick masonry after fire exposure. Compressive strength tests of the mortar, clay perforated brick, and perforated brick masonry specimens were performed in accordance with ISO834 fire tests of different durations. The temperature distribution of the masonry materials and specimens was simulated using the finite element software ABAQUS, with the thermal parameters of masonry materials recommended by European standard Eurocode 6 and related literature. The compressive strength reduction factors of mortar and clay perforated brick exposed to different fire durations were calculated via the layered method suggested by European standard Eurocode 1. In addition, the compressive strength reduction factors after cooldown were obtained from the experimental data of the masonry materials, and by considering further reductions in the compressive strength after cooling from high temperatures. Experimental data of the masonry specimens were compared with the numerical results obtained using the reduction factors proposed in this work. The comparison revealed an overall acceptable approximation. Thus, the method presented in this paper can be used to evaluate the residual capacity of masonry structures after fire.     

胸腺五肽辅助治疗肺癌对免疫功能影响及其疗效的系统评价

为了系统地评价胸腺五肽作为辅助药物治疗各种肺癌的疗效及其对机体免疫功能的影响，利用电子检索收集有关胸腺五肽联合放疗或化疗方案治疗肺癌的临床随机对照试验文献，对符合纳入标准的文献，采用RevMan5.3 软件进行系统评价。最终共纳入文献 9 篇，总样本量 784 例。Meta 分析结果表明，胸腺五肽作为辅助药物治疗各种肺癌提高总有效率的差异无统计学意义[OR ＝ 1.44, 95%CI(0.99, 2.10), P ＝0.06 ＞ 0.05]。在对免疫功能的影响方面，胸腺五肽的使用显著增高外周血中的 CD3+ 细胞水平[OR ＝ 5.88, 95% CI(2.34, 9.42), P ＝0.001]，CD4+ 细胞水平也显著上升[OR ＝8.32, 95%CI(5.22, 11.42), P ＜ 0.00001] , CD4＋ /CD8＋比值也有明显的提高[OR ＝ 0.38, 95% CI(0.18, 0.59), P＝0.0002]，但 CD8+ 细胞水平的差异无统计学意义[OR ＝－3.12, 95% CI ( －9.02, 2.79), P ＞0.05]。总的来说，本研究在一定程度上反映了在辅助治疗肺癌方面，胸腺五肽能显著提高外周血中的 CD3+ 细胞水平、CD4+ 细胞水平、CD4+/CD8+ 比值。而对于治疗的有效率、CD8+ 细胞水平，差异无统计学意义。