Oxidant-Resistant Hydrogen-Bond-Donating Organocatalyst for Enantioselective Nucleophilic Epoxidation of α,β-Unsaturated Amides

Bifunctional benzothiadiazine-catalyzed epoxidation of α, β-unsaturated amides proceeds efficiently to give chiral 2-oxiranecarboxamides in excellent yields of 89–99 % and with good enantioselectivity of up to 84 % ee. A synthetic application of the oxiranecarboxamides is also described

Citrinin Derivatives From Penicillium Citrinum Y34 That Inhibit α-Glucosidase and ATP-Citrate Lyase

Two new citrinin dimers bearing a 6,6-spiroketal moiety (1 and 2) and four known analogues (3–6), together with 18 known citrinin monomers (7–24), were isolated from the culture of hydrothermal vent-associated fungus Penicillium citrinum Y34. Their structures were identified by extensive spectroscopic analyses, 13C NMR calculation in combination with DP4+, linear correlation coefficient (R2), and mean absolute error (MAE) values analyses, and electronic circular dichroism (ECD) calculation. The α-glucosidase and ATP-citrate lyase (ACL) inhibitory activities of isolated compounds were evaluated. Compounds 1, 3, and 12 displayed moderate α-glucosidase inhibitory activities with IC50 values of 239.8, 176.2, and 424.4 μM, respectively. Enzyme kinetics investigations of 1 and 3 suggested their non-competitive inhibition of α-glucosidase with Ki values of 204.3 and 212.7 μM, respectively. Meanwhile, compound 4 showed significant ACL inhibitory potential with an IC50 value of 17.4 μM. Furthermore, the interactions of 1, 3, and 12 with α-glucosidase and 4 with ACL were investigated by molecular docking assay. This study demonstrates that citrinins, especially for their dimers, could be potential lead compounds for the development of new agents for the treatment of metabolic diseases

貧困層の疾患を解決するための総合的アプローチ-マラリアを例として-

京都大学0048新制・課程博士博士(総合学術)甲第21231号総総博第3号新制||総総||1(附属図書館)京都大学大学院総合生存学館総合生存学専攻(主査)教授 竹本 佳司, 特定教授 大嶌 幸一郎, 教授 大野 浩章学位規則第4条第1項該当Doctor of PhilosophyKyoto UniversityDFA

Disturbed Sites Junction

Situated along the Mississippi River at the head of the North Riverfront Recreational Trail and about 1 mile north of St. Louis’ Gateway Arch grounds, the post-industrial site for this studio is a confluence of industry and invention, of abandonment, neglect, contemporary relevance, and future potential. Spanning approximately 30 acres, it is bordered on the east side by the Mississippi River, on the north by the Corrections Department Work-Release Center on Mullanphy Street, on the south by the Laclede Power Station, and on the west by the historic Cotton Belt Freight Depot. Highway 70 lies 3 blocks west of the site; a rail line also passes through the west end. There is a major opening in the floodwall at the crossing of Mullanphy and Commercial Streets. Throughout the years, the site has been a haven to a number of transient and/or homeless groups. Currently, it is home to a significant tent city. The ultimate charge of the studio is to reclaim and transform the site into a public landscape that recognizes the relationships between city and river, and between static and fluid spaces, taking into account past, present, and future uses.https://openscholarship.wustl.edu/fall2010_yates/1001/thumbnail.jp

Organocatalytic direct α-selective N-glycosylation of amide with glycosyl trichloroacetimidate

Through the synergistic catalytic effect of the halogen bond (XB) donor and thiourea catalyst, a direct α-selective N-glycosylation of the amide residue of asparagine derivative was achieved using readily accessible glycosyl trichloroacetimidate. n-Butyl methyl ether was found to be the most suitable solvent for the α-selectivity

An Integrated Approach to Combat Diseases of Poverty: Malaria as an Example

学位プログラム名: 京都大学大学院思修

circ-TFRC downregulation suppresses ovarian cancer progression via miR-615-3p/IGF2 axis regulation

Abstract Background Ovarian cancer (OC) is a malignancy among female globally. Circular RNAs (circRNAs) are a family of circular endogenous RNAs generated from selective splicing, which take part in many traits. Former investigation suggested that circ-TFRC was abnormally expressed in breast cancer (BC). Further, the role of circ-TFRC to the progress of OC remains unclear. So, the aim of this study was to reveal the regulatory mechanism of circ-TFRC. Methods Our team made the luciferase reporter assay to validate circ-TFRC downstream target. Transwell migration assay, 5-ethynyl-20-deoxyuridine, and cell counting kit-8 were applied to investigate both proliferation and migration. In vivo tumorigenesis and metastasis assays were performed to investigate the circ-TFRC role in OC. Results The outputs elucidated that circ-TFRC expression incremented in OC cells and tissues. circ-TFRC downregulation inhibited OC cell proliferation as well as migration in in vivo and in vitro experiments. The luciferase results validated that miR-615-3p and IGF2 were circ-TFRC downstream targets. IGF2 overexpression or miR-615-3p inhibition reversed OC cell migration after circ-TFRC silencing. Also, IGF2 overexpression reversed OC cell migration and proliferation post miR-615-3p upregulation. Conclusion Results demonstrate that circ-TFRC downregulation inhibits OC progression and metastasis via IGF2 expression regulation and miR-615-3psponging

Information Security of PHY Layer in Wireless Networks

Since the characteristics of wireless channel are open and broadcasting, wireless networks are very vulnerable to be attacked via eavesdropping, jamming, and interference. As traditional secure technologies are not suitable for PHY layer of wireless networks, physical-layer security issues become a focus of attention. In this paper, we firstly identify and summarize the threats and vulnerabilities in PHY layer of wireless networks. Then, we give a holistic overview of PHY layer secure schemes, which are divided into three categories: spatial domain-based, time domain-based, and frequency domain-based. Along the way, we analyze the pros and cons of current secure technologies in each category. In addition, we also conclude the techniques and methods used in these categories and point out the open research issues and directions in this area