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Differential effect of various inhibitors on four types of rat sialidase

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Abstract

The inhibitory effect of various compounds on the activities of four types of rat sialidase was investigated. 2-Deoxy-2,3-dehydro-N-acetylneuraminic acid andN-acetylneuraminic acid were competitive inhibitors for the sialidases. The former was effective against cytosolic sialidase and intralysosomal sialidase more than two membrane-associated sialidases I and II, the latter being a much weaker inhibitor. A heavy metal ion such as Cu2+ (1mm) and thiol-modifying 4-hydroxymercuribenzoate (50 µm) caused complete inhibition of the activities of cytosolic sialidase and membrane sialidase I, while no decrease in the activities of intralysosomal sialidase and membrane sialidase II was observed. When 4-nitrophenyloxamic acid and siastatin B, inhibitors of bacterial sialidases, and synthetic thioglycoside GM3 analogue Neu5Acα-s-(2-6)Galβ(1-4)Glcβ(1-1) ceramide, an inhibitor of influenza virus sialidase, were tested, they did not affect any activity of the rat sialidases. By the differential effect of these inhibitors, the four types of rat sialidase could be discriminated from one another and furthermore from viral and bacterial sialidases.

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Abbreviations

Neu5Ac:

N-acetylneuraminic acid

Neu5Ac2en:

2-deoxy-2,3-dehydro-N-acetylneuraminic acid

4MU-Neu5Ac:

4-methylumbelliferyl-α-N-acetyl-d-neuraminic acid

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Authors and Affiliations

  1. Division of Biochemistry, Research Institute, Miyagi Cancer Center, 47-1 Nodayama, Medeshima-Shiode, Natori-shi, 981-12, Miyagi-ken, Japan

    Taeko Miyagi & Keiko Hata

  2. Department of Applied Bio-organic Chemistry, Gifu University, 501-11, Gifu, Japan

    Akira Hasegawa

  3. Institute of Microbial Chemistry, Kamiosaki, Shinagawa-ku, 141, Tokyo, Japan

    Takaaki Aoyagi

Authors
  1. Taeko Miyagi
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  2. Keiko Hata
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  3. Akira Hasegawa
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  4. Takaaki Aoyagi
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Miyagi, T., Hata, K., Hasegawa, A. et al. Differential effect of various inhibitors on four types of rat sialidase. Glycoconjugate J 10, 45–49 (1993). https://doi.org/10.1007/BF00731186

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  • DOI: https://doi.org/10.1007/BF00731186

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