83 research outputs found

    Structural basis for potent inhibition of d-amino acid oxidase by thiophene carboxylic acids

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    A series of thiophene-2-carboxylic acids and thiophene-3-carboxylic acids were identified as a new class of DAO inhibitors. Structure-activity relationship (SAR) studies revealed that small substituents are well-tolerated on the thiophene ring of both the 2-carboxylic acid and 3-carboxylic acid scaffolds. Crystal structures of human DAO in complex with potent thiophene carboxylic acids revealed that Tyr224 was tightly stacked with the thiophene ring of the inhibitors, resulting in the disappearance of the secondary pocket observed with other DAO inhibitors. Molecular dynamics simulations of the complex revealed that Tyr224 preferred the stacked conformation irrespective of whether Tyr224 was stacked or not in the initial state of the simulations. MM/GBSA indicated a substantial hydrophobic interaction between Tyr244 and the thiophene-based inhibitor. In addition, the active site was tightly closed with an extensive network of hydrogen bonds including those from Tyr224 in the stacked conformation. The introduction of a large branched side chain to the thiophene ring markedly decreased potency. These results are in marked contrast to other DAO inhibitors that can gain potency with a branched side chain extending to the secondary pocket due to Tyr224 repositioning. These insights should be of particular importance in future efforts to optimize DAO inhibitors with novel scaffolds

    Development of a Multifunctional Lightweight Membrane with a High Specific Power Generation Capacity

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    As a lighter power generation system, Japan Aerospace Exploration Agency (JAXA) and Sakase Adtech Corp. are developing a demonstrator component named “Harvesting Energy with Lightweight Integrated Origami Structure” (HELIOS), which is a deployable lightweight membrane structure. HELIOS has solar arrays on its surface and demonstrates the technology which enables higher specific power generation capacity compared to the conventional solar array panels. The membrane also has communication antennas, showing the potency of lightweight membrane’s multifunctionality such as large data transmitting by 5G antennas and high-resolution observation by interferometer antennas. This paper presents the component’s concept and design, and the expected achievements

    The Japanese Clinical Practice Guideline for acute kidney injury 2016

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    Acute kidney injury (AKI) is a syndrome which has a broad range of etiologic factors depending on different clinical settings. Because AKI has significant impacts on prognosis in any clinical settings, early detection and intervention are necessary to improve the outcomes of AKI patients. This clinical guideline for AKI was developed by a multidisciplinary approach with nephrology, intensive care medicine, blood purification, and pediatrics. Of note, clinical practice for AKI management which was widely performed in Japan was also evaluated with comprehensive literature search

    ニューパルツ学術訪問団報告記

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    平成14年3月19日から4月2日までの日程で,計22名から構成されたニューパルツ学術訪問団が派遣された。今回の学術訪問団派遣は同時に研修旅行の意味合いも持ち,滞在中に施設訪問や英会話研修も行った。ここに記念すべき第1回の新見公立短期大学のニューパルツヘの学術訪問団派遣についてまとめ,今後の両大学の交流に役立てたい

    Introducing Dual Regularization Parameters into Regularized Channel Inversion (RCI)-Based Vector Perturbation for Modulo Loss Reduction

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    Abstract—This paper proposes a method to reduce the symbol error caused by modulo operator for regularized channel inversion (RCI)-based vector perturbation (RCI-VP). The proposed method introduces dual regularization parameters of RCI precoding matrix. First regularization parameter α1 is set so as to maximize the signal to interference plus noise ratio (SINR) value of each stream to find the optimal perturbation vector. The second regularization parameter α2 is set so as to minimize the total MSE between the transmitted perturbation vector and received perturbation vector to reduce the symbol error caused by modulo operator. The simulated results confirm that the proposed method can improve the performance of RCI-VP over i.i.d. MIMO channel and frequency-selective fading MIMO channel. Keywords—Vector perturbation, SINR maximization, Modulo loss, Regularization parameter, Minimum mean square error I
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