摘要：Dipeptidyl peptidase 4(DPP-4)is a clinically validated target for the treatment of type 2 diabetes mellitus(T2DM).To discover novel and potent DPP-4 inhibitors,three series of compounds were designed and synthesized in this study based on our previously identified novel scaffold of 2-phenyl-3,4-dihydro-2H-benzo[f]*** the designed compounds,41d-1 was the most po tent one with an IC_(50) value of 16.00 nM.

摘要：Local hydrodynamics of a gas–liquid–solid system,such as bubble circulation regime,gas holdup,liquid velocity and axial profile of solid concentration,are studied in a two-stage internal loop airlift *** correlations for gas holdup and liquid velocity are proposed to ease the reactor design and *** bubble circulation regimes were displayed in the first(lower) and second(upper) *** superficial gas velocity and solid loading can promote regime transition of the second stage,and the gas holdup of the second stage is higher than that of the lower *** addition,the effects of solid loading on bubble behaviour are experimentally investigated for each *** is found that bubble size in the downcomer decreases with the presence of solid particles,and bubble size distribution widens under higher superficial gas velocity and lower solid loading.

摘要：We propose a thoroughly optimal signal design strategy to achieve the Pareto boundary （boundary of the achievable rate region） with improper Gaussian signaling （IGS） on the Z-interference channel （Z-IC） under the assumption that the interference is treated as additive Gaussian noise. Specifically, we show that the Pareto boundary has two different schemes determined by the two paths manifesting the characteristic of improperly transmitted signals. In each scheme, we derive several concise closed-form expressions to calculate each user＇s optimally transmitted power, covariance, and pseudo-covariance of improperly transmitted signals. The effectiveness of the proposed optimal signal design strategy is supported by simulations, and the results clearly show the superiority of IGS. The proposed optimal signal design strategy also provides a simple way to achieve the required rate region, with which we also derive a closed-form solution to quickly find the circularity coefficient that maximizes the sum rate. Finally, we provide an in-depth discussion of the structure of the Pareto boundary, characterized by the channel coefficient, the degree of impropriety measured by the covariance, and the pseudo-covaxiance of signals transmitted by two users.

摘要：从1950年10月25日至1958年10月26日,中国人民志愿军在朝鲜直接作战近3年、留驻5年,表明了彼时国际秩序的不稳定。相对于抗日战争反侵略、反殖民、反压迫的被动属性,朝鲜战争无疑更具主动性。中国人民通过战争表现出的决心、勇气,以及取得的最后胜利。

摘要：微纳机器人(MNR)也称微纳马达,是一种可自主运动的微纳功能器件.作为一个全新的交叉研究领域,MNR在生物医学、环境修复和微纳制造等多个领域展现出巨大的应用潜力.MNR通常依赖于非对称的结构设计[1],并通过转化外界的声、光、电、热、磁和化学能等能量来进行自驱动[2~6].这些非对称结构可通过材料定向真空沉积、模板电沉积和原位合成等方法实现.然而,如何根据应用需求进行理性的可设计性定制微纳机器人仍然是一个亟待解决的难题.

摘要：先导化合物的设计和发现是新药研发中最具挑战性和创造性的阶段,其过程需考虑候选分子的结构新颖性、生物活性、靶标选择性、可合成性、成药性和安全性等多种属性的优化.虽然计算机辅助药物设计方法的发展和应用大大节省了先导化合物发现阶段的时间和经济成本,但仍未能扭转新药研发成功率低的现状.近年来,随着深度学习技术的不断发展,基于深度学习的全新药物设计方法为先导化合物的发现带来新的契机,前景巨大.这些全新药物设计模型使用的深度学习框架包括编码-解码器、循环神经网络、生成对抗网络、强化学习等.本文综述了这些深度学习框架的基本原理、模型输入分子表征以及效果评测指标,并对其在全新药物设计领域的应用前景进行了展望.

摘要：1991年诺贝尔文学奖获得者纳丁·戈迪默是南非的国宝级作家。她虽为白人,却有着鲜明的“非洲中心意识”,始终深扎南非进行文学创作。在其70年的文学创作生涯中,戈迪默一直都致力于构建出富有主体性、民族性和革命性的本土化艺术表达。戈迪默的本土化文学书写,不论是早期的民族主体意识构建,中期的激进主义叙事策略,还是后期的家国理念重塑,都生动呈现了南非人民的百味人生和南非历史的百年变迁,启迪着南非人民挣脱非自然历史的奴役和异化,成长为具有主体意识和民族意识的公民,成为保存南非民族历史记忆、捍卫非洲文化传统和守护非洲人文主义价值观的“自然资源保护者”。

摘要：深部巷道大变形已成为深部煤炭安全高效开采的关键制约因素。为实现深部软弱围岩稳定性控制,提出了基于深部巷道大变形演化过程的分步联合支护方案及其理论分析模型。结果表明,深部软弱围岩呈破裂碎胀变形-损伤扩容变形-连续变形的分布特征。分步联合支护后,围岩极限承载力随锚杆和锚索等效支护力增大呈线性增大趋势,但随注浆修复系数呈指数增大趋势。锚杆和锚索支护设计时应以极限承载力所需的注浆修复系数等于1.0时的等效支护力临界条件为基准。深浅孔注浆支护时须同时考虑注浆修复系数和围岩破裂区半径。不同支护措施的协同支护参数可由破裂修复区围岩极限承载平衡条件确定。数值模拟和工程应用分析表明,分步联合支护可实现深部软弱围岩碎胀大变形控制,具有较高的工程推广应用价值。

摘要：异体材料表面引起血栓形成是限制血液接触器件成功应用的主要问题之一.传统的表面抗血栓改性策略主要基于"抑制纤维蛋白(初级血栓)形成"这一基本设计思路,然而大量实践证明,异体材料在接触血液时,凝血反应是不可避免的.纤溶表面的概念突破了传统抗血栓思路,从"溶解纤维蛋白"的角度设计材料表面,使其在接触血液环境时,充分调动人体纤溶系统,从而迅速溶解初步形成但尚未对人体造成危害的血栓.在过去十几年中,以加拿大麦克马斯特大学的Brash课题组以及作者课题组为代表的研究团队们已经充分证实了纤溶表面这一概念的可行性,并发展了多种构建纤溶表面的方法.本专论详细介绍了这些研究进展,并展望了该领域未来的发展方向,旨在激发更多的研究者关注这个尚未全面开发但却极具潜力和重要性的材料表面抗血栓的新概念和新方法,进而推动其实现在血液接触器件方面的成功应用.

摘要：The 5＇-flanking proximal region of stress-induced gene encoding choline monooxygenase （CMO） was isolated by Adaptor-PCR and TAIL-PCR from halophyte Suaeda liaotungensis K. A total of 2,204 bp DNA sequence was obtained. The transcription start site, which is located at 128 bp upstream to the start ATG, was predicted by the TSSP-TCM program. The functional elements were analysed by PLACE program. The obtained SICMO gene promoter contains the basic elements： TATA-box, CAAT-box, and stress-induced elements, for example, salt responsive element （GAAAAA）, cold responsive elements （CANNTG）, ABA （Abscisic Acid） responsive elements （NAACAA）, water stress element （CGGTTG）, and WUN responsive elements （GTTAGGTTC）. Isolation and analysis of the promoter of the CMO gene from S. liaotungensis lays a foundation for characterising the stress-induced promoter elements, studying the relationship between the structure and function of the promoter, and investigating the molecular mechanism of CMO gene regulation.