93 research outputs found

    A high precision and low noise S/H circuit design for video signal sampling

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    Secured green communication scheme for interference alignment based networks

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    In this paper, a new security and green communication scheme is proposed to the Interference-Alignment (IA) based networks. To achieve a secured communication, full-duplex receivers are utilized to transmit artificial noise (AN). Both the signals and the ANs are used to harvest energy to realize green communication. For these reasons, the feasible conditions of this scheme are analyzed first. Secondly, the average transmission rate, the secrecy performance and the harvested energy are investigated. Thirdly, an optimization scheme of simultaneous wireless information and power transfer (SWIPT) is given to optimize the information transmission and the energy harvesting efficiency. Meanwhile, an improved IA iteration algorithm is designed to eliminate both the AN and the interference. Furthermore, relay cooperation is considered and its system performance is analyzed. The simulations show that the target average transmission rate is not affected by AN, while the secrecy performance can be greatly improved. The energy harvesting efficiency is also better than the traditional schemes. As expected, the average transmission rate further is improved with the relay cooperation

    Structure-Activity Relationship Study Enables the Discovery of a Novel Berberine Analogue as RXRα Activator to Inhibit Colon Cancer

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    黄连素是从黄连、黄柏等传统中药中提取的单体化合物,常用于治疗痢疾及其它消化道感染。近年来,黄连素的抗心律失常、调控能量代谢、降血糖血脂和抗癌等多重功效使其成为一个“明星”中药单体化合物。尽管黄连素具有很好的安全性,但其抗癌作用在临床应用上仍具有许多局限性,包括抗癌活性低、溶解度和生物利用度低等。然而,由于黄连素的分子靶点不清楚,以往对黄连素的改造比较盲目和随机,并未取得较好的进展。胡天惠团队与张延东团队紧密合作、优势互补,针对黄连素与RXR的结合模式,运用结构生物学方法和全合成相结合,设计合成了多种黄连素衍生物,并开展了构效关系分析。发现黄连素衍生物B-12在结合并激活RXR、抗肠癌活性、溶解度和生物利用度方面均明显优于黄连素,且保留了黄连素的肿瘤选择性和低毒副作用,具有很好的临床转化前景。该研究也为结构生物学指导黄连素衍生物药物设计提供了理论基础。本论文的通讯作者为医学院占艳艳副教授、张延东教授和胡天惠教授。医学院博士生徐贝贝和化学化工学院博士生江训金为共同第一作者。We reported recently that berberine, a traditional oriental medicine to treat gastroenteritis, binds and activates Retinoid X receptor α (RXRα) to suppress the growth of colon cancer cells. Here, we extended our studies based on the binding mode of berberine with RXRα by design, synthesis and biological evaluation of a focused library of 15 novel berberine analogues. Among them, 3,9-dimethoxy-5,6-dihydroisoquinolino[3,2-a]isoquinolin-7-ium chloride (B-12) was identified as the optimal RXRα activator. More efficiently than berberine, B-12 bound and altered the conformation of RXRα/LBD, thereby suppressing Wnt/β-catenin pathway and colon cancer cell growth via RXRα mediation. In addition, B-12 not only preserved berberine’s tumor selectivity but also greatly improved its bioavailability. Remarkably, in mice, B-12 did not show obvious side effects including hypertriglyceridemia as other RXRα agonists, or induce hepatorenal toxicity. Together, our study describes an approach for the rational design of berberine-derived RXRα activators as novel effective antineoplastic agents for colon cancer.This work was supported by the National Natural Science Foundation of China (31770860, 21772164, 81572589, 81602560 and 21572187), and the Natural Science Foundation of Fujian Province (2018R1036-2, 2017J06020, 2019R1001-4, and 2019R1001-5). 项目得到了国家自然科学基金委促进海峡两岸科技合作联合基金重点项目、面上项目和福建省自然科学基金的支持

    ULK1 phosphorylates Exo70 to suppress breast cancer metastasis

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    乳腺癌是威胁女性生命健康的“头号杀手”,而远处转移是乳腺癌患者死亡的主要原因。因此,了解乳腺癌如何发动侵袭和转移,对于有效治疗乳腺癌、延长病人生存期具有重要意义。本研究中,该团队发现ULK1通过结合并磷酸化胞泌蛋白复合体关键亚基Exo70来抑制乳腺癌转移。ULK1对Exo70上Ser47,Ser59和Ser89位点的磷酸化,严重地削弱了Exo70的自身寡聚化和与其它胞外分泌复合体亚基的结合,进而减少了细胞运动伪足形成以及基质金属蛋白酶的分泌,从而抑制乳腺癌细胞的迁移和侵袭。该论文首次揭示了胞外分泌复合体重要成员Exo70在乳腺癌中受到ULK1和ERK1/2的双重磷酸化调控,从而使得乳腺癌细胞可以根据外环境来决定潜伏还是发动侵袭转移,为乳腺癌的治疗提供了新的理论基础。 本论文的通讯作者为占艳艳副教授、郭巍教授和胡天惠教授。医学院博士生毛丽媛、占艳艳副教授、吴斌博士和医学院博士生于强为共同第一作者。【Abstract】Increased expression of protein kinase ULK1 was reported to negatively correlate with breast cancer metastasis. Here we report that ULK1 suppresses the migration and invasion of human breast cancer cells. The suppressive effect is mediated through direct phosphorylation of Exo70, a key component of the exocyst complex. ULK1 phosphorylation inhibits Exo70 homo-oligomerization as well as its assembly to the exocyst complex, which are needed for cell protrusion formation and matrix metalloproteinases secretion during cell invasion. Reversely, upon growth factor stimulation, Exo70 is phosphorylated by ERK1/2, which in turn suppresses its phosphorylation by ULK1. Together, our study identifies Exo70 as a substrate of ULK1 that inhibits cancer metastasis, and demonstrates that two counteractive regulatory mechanisms are well orchestrated during tumor cell invasion.This work was supported by the grants from the National Natural Science Foundation of China (81572589, U1405228, 81472568, and 31770860), the Natural Science Foundation of Fujian grant (2017J06020, 2018J01400, 2017R1036-4, 2017R1036-6, 2016R1034-1, and 2016R1034-4), and the Xiamen Science and Technology grant (3502Z20159013) to Y.-y.Z. and T.H., and National Institute of Health R01 GM111128 to W.G.该论文的研究成果是在国家自然科学基金和福建省基金的资助下,与美国宾夕法尼亚大学和清华大学共同协作完成的

    A New Series of Three-Dimensional Chaotic Systems with Cross-Product Nonlinearities and Their Switching

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    This paper introduces a new series of three-dimensional chaotic systems with cross-product nonlinearities. Based on some conditions, we analyze the globally exponentially or globally conditional exponentially attractive set and positive invariant set of these chaotic systems. Moreover, we give some known examples to show our results, and the exponential estimation is explicitly derived. Finally, we construct some three-dimensional chaotic systems with cross-product nonlinearities and study the switching system between them

    Recent Advances in Dynamic Kinetic Resolution by Chiral Bifunctional (Thio)urea- and Squaramide-Based Organocatalysts

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    The organocatalysis-based dynamic kinetic resolution (DKR) process has proved to be a powerful strategy for the construction of chiral compounds. In this feature review, we summarized recent progress on the DKR process, which was promoted by chiral bifunctional (thio)urea and squaramide catalysis via hydrogen-bonding interactions between substrates and catalysts. A wide range of asymmetric reactions involving DKR, such as asymmetric alcoholysis of azlactones, asymmetric Michael–Michael cascade reaction, and enantioselective selenocyclization, are reviewed and demonstrate the efficiency of this strategy. The (thio)urea and squaramide catalysts with dual activation would be efficient for more unmet challenges in dynamic kinetic resolution

    A general and facile one-pot process of isothiocyanates from amines under aqueous conditions

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    A general and facile one-pot protocol for the preparation of a broad range of alkyl and aryl isothiocyanates has been developed from their corresponding primary amines under aqueous conditions. This synthetic process involves an in situ generation of a dithiocarbamate salt from the amine substrate by reacting with CS2 followed by elimination to form the isothiocyanate product with cyanuric acid as the desulfurylation reagent. The choice of solvent is of decisive importance for the successful formation of the dithiocarbamate salt particularly for highly electron-deficient substrates. This novel and economical method is suitable for scale-up activities
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