國家衛生研究院 NHRI:Item 3990099045/8599
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    题名: Development and application of a fluorescent glucose uptake assay for the high-throughput screening of non-glycoside SGLT2 inhibitors
    作者: Wu, SH;Yao, CH;Hsieh, CJ;Liu, YW;Chao, YS;Song, JS;Lee, JC
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors are of current interest as a treatment for type 2 diabetes. Efforts have been made to discover phlorizin-related glycosides with good SGLT2 inhibitory activity. To increase structural diversity and better understand the role of non-glycoside SGLT2 inhibitors on glycemic control, we initiated a research program to identify non-glycoside hits from high-throughput screening. Here, we report the development of a novel, fluorogenic probe-based glucose uptake system based on a Cu(I)-catalyzed [3 + 2] cycloaddition. The safer processes and cheaper substances made the developed assay our first priority for large-scale primary screening as compared to the well-known [14C]-labeled α-methyl-D-glucopyranoside ([14C]-AMG) radioactive assay. This effort culminated in the identification of a benzimidazole, non-glycoside SGLT2 hit with an EC50 value of 0.62 μM by high-throughput screening of 41,000 compounds.
    日期: 2015-07
    關聯: European Journal of Pharmaceutical Sciences. 2015 Jul;74:40-44.
    Link to: http://dx.doi.org/10.1016/j.ejps.2015.03.011
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0928-0987&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000355711400006
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84928499272
    显示于类别:[李靜琪] 期刊論文
    [趙宇生(2002-2013)] 期刊論文

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