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Rapid Diversity-Oriented Synthesis in Microtiter Plates for In Situ Screening: Discovery of Potent and Selective α-Fucosidase Inhibitors

Authors

  • Chung-Yi Wu Dr.,

    1. The Genomics Research Center and, Institute of Biological Chemistry, Academia Sinica, No. 128 Academia Road Section 2, Nan-Kang, Taipei, 11529, Taiwan, Fax: (+886) 2-2651-4705
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  • Chuan-Fa Chang Dr.,

    1. The Genomics Research Center and, Institute of Biological Chemistry, Academia Sinica, No. 128 Academia Road Section 2, Nan-Kang, Taipei, 11529, Taiwan, Fax: (+886) 2-2651-4705
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  • Jenny Szu-Yu Chen,

    1. The Genomics Research Center and, Institute of Biological Chemistry, Academia Sinica, No. 128 Academia Road Section 2, Nan-Kang, Taipei, 11529, Taiwan, Fax: (+886) 2-2651-4705
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  • Chi-Huey Wong Prof.,

    1. The Genomics Research Center and, Institute of Biological Chemistry, Academia Sinica, No. 128 Academia Road Section 2, Nan-Kang, Taipei, 11529, Taiwan, Fax: (+886) 2-2651-4705
    2. Department of Chemistry and, the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA, Fax: (+1) 858-784-2409
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  • Chun-Hung Lin Prof.

    1. The Genomics Research Center and, Institute of Biological Chemistry, Academia Sinica, No. 128 Academia Road Section 2, Nan-Kang, Taipei, 11529, Taiwan, Fax: (+886) 2-2651-4705
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  • This work was supported by Academia Sinica, Taipei, Taiwan.

Abstract

original image

Eine effiziente und einfache Methode im Mikrotiterplattenformat zur Identifizierung potenter und selektiver Inhibitoren von α-Fucosidasen wurde entwickelt. Sie beruht auf der Amidbildung einer Fuconojirimycin-Kernstruktur mit Carbonsäuren und anschließendem Inhibierungs-Assay ohne Isolierung des Produkts. Gezeigt sind die Strukturen der beiden potentesten Inhibitoren.

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