摘要：Peptide stapling strategy has been proven a promising solution in addressing two major pharmacological hurdles, proteolytic stability and membrane permeability, for small peptides as therapeutics. This stapling peptides feature a covalent cross-link of side chains, thus effectively mimicking α-helix as inhibitors of protein-protein interactions. In this review, we category and analyze key examples of various peptide stapling strategies based on different cross-links aligned on the side chain of peptides mainly in the last three years.

摘要：Based on the active site of lanosterol 14α-demethylase of azole antifungal agents,sixteen 1-（1H-1,2,4-triazole-1-yl）- 2-（2,4- difluorophenyl）-3-（N-n-butyl-N-1-substitutedbenzyl-4-methylene-1H-1,2,3-triazole）-2-propanols have been designed,synthesized and evaluated as antifungal *** of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that some of the compounds exhibited excellent activities with broad spectrum.

摘要：Twenty-three 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase. In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

摘要：A series of 1-（1H-1,2,4-triazole-1-yl）-2-（2,4-difluoropheny1）-3-（N-isoproy1-N-substituted-amino）-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase （CYP51）. Their structures were confirmed by MS and ^1H NMR. In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi. The results showed that all title compounds exhibited activity against fungi tested to some extent. Compounds 3c, 3d, 7a, 7b and 7e exhibited more potent antifungal activities against nearly all fungi tested except AspergiUus fumigatus than fluconazole. ？2009 Qiu Ye Wu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All fights reserved.

摘要：According to the structure features of Fe80P20, A series of clusters Fe4P were designed and focused on studying the stability of local structure, charge distribution and chemical bond, Using the DFT method, energy and structure of Fe4P clusters were optimized and analyzed. The computational results showed that the energy of cluster 1（2） has the lowest energy, and the possibility of its existence in the Fe80P20 is high. Analyzing the transition states among the clusters, it was found that the clusters in the doublet state are more stable than those in the quartet state. The numbers of the Fe-P bond in the clusters play important roles in the cluster stability and electrons transfer properties, The more numbers of Fe-P bonds in the clusters, the higher the cluster stability, and the weaker the ability of P atom to get electron, The number of Fe atoms, which has bonding interactions with the P atom, is direct proportional to the average 3d orbit population of Fe atom. Basing on the orbital population, average magnetic moments of each Fe atom in the Fe4P clusters were calculated, and they are all smaller than that of single metal Fe atom. This suggests that all Fe4P clusters have soft magnetic property and they are expected to be perfect material for preparing soft magnetic apparatus.

摘要：为了研究负泊松比(negative Poisson's ratio,NPR)锚索在静力拉伸和落锤冲击荷载作用下的力学特性,采用自主研发的NPR锚索拉力实验系统和NPR锚索落锤冲击实验系统对NPR锚索进行静力拉伸试验以及动力冲击实验。从锚索的支护力、锚索伸长量以及膨胀量等方面验证了其抵抗和吸收围岩缓慢变形、瞬时冲击能量的性能。其次,建立了NPR锚索三维数值模型,并根据室内试验结果标定了相关数值参数。开展了NPR锚索静力拉伸数值试验以及落锤冲击数值试验,数值试验结果与室内试验结果一致性较好,验证了数值模型的可靠性。该NPR锚索三维数值模型可作为NPR锚索的改进和升级换代的辅助分析工具。

摘要：由于当前已有系统未能建立精准化采购模型,导致系统管理成本和管理复杂度增加,管理效率下降,提出一种基于信息共享平台的精准化采购物资管理系统。结合ERP理念,结合采购物资和先进信息,设计系统总体框架,同时分别介绍不同模块的功能。在信息共享平台下,依据模糊理论分析采购管理过程中的不确定性,建立决策需求和订货费均为模糊参数的精细化采购决策模型。通过符号距离以及重心法进行模糊值优化,确定最佳订货期以及采购量。仿真实验结果表明,所设计系统能显著降低管理开销与复杂性,同时大幅提升管理效能。

摘要：视频孪生是将视频与数字孪生融合的技术体系,是对数字孪生的实时实景升级。将视频孪生技术用在水利工程中,能提升水利工程的建设效率和管理水平,赋能国家水利工程建设和保证水利基础设施的安全,实现较好的经济效益、社会效益和生态效益。论文提出了一种基于视频孪生技术的水利工程数字化管理平台,核心技术为三维地理信息引擎,通过整合云计算、大数据、人工智能、遥感、数字仿真等先进技术,实现流域全要素的数字映射与实时动态监控。该平台以视频孪生为核心,融合“3DGIS+BIM+Video”技术,能够将大规模实时监控视频与地理信息进行时空统一,从而解决了传统监控视频位置不明确、画面分散不直观等问题,提升了水利工程现场态势的精准掌控与直观管理。论文所提出的水利工程视频孪生技术架构不仅提升了水利工程的监测精度与管理效率,也为水利行业的数字化、智能化转型提供了重要支撑。

摘要：针对既能通过通用移动存储设备将非涉密计算机中的数据导入涉密计算机,又能防止涉密计算机中的信息通过通用移动存储设备泄露的问题,设计了一种基于数据二极管的移动存储设备数据安全导入系统。给出了该系统的硬件和软件设计,创新性地将数据二极管技术应用于移动存储设备的数据导入。介绍了基于双光纤收发器实现数据二极管的方法,详细分析了影响数据导入可靠性的几种因素,提出了"分片重传"、"分片写盘"等提高数据导入可靠性的方法。给出的方法能有效提高数据导入的可靠性,对于安全导入系统的具体实现具有重要的参考价值。

摘要：目的 运用“在地性”理念探索上海泗泾古镇文化符号的设计与研究。方法 以“在地性”的提出与研究现状为基础,总结在地设计的内涵与特征,提出以“人”的感知为核心,以“地”的文化为依托、以“物”的设计为表达的应用思路。通过上海泗泾古镇文化符号的在地性设计实践,解析了从在地感知调研,到在地文化符号选取与转化,再到在地文化衍生设计的方法与过程。结果 成为将设计者置于研究地域内,与当地文化视为一体,并作出设计反馈的生动案例。结论 是推动上海泗泾古镇文化的传承与推广,用现代设计构筑美好生活,从“文化自信”的视角使传统古镇文化“活起来”的一次积极探索。