Inactivation of bleomycin by an N-acetyltransferase in the bleomycin-producing strain Streptomyces verticillus

Authors

  • Masanori Sugiyama,

    Corresponding author
    1. Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Kasumi 1-2-3, Minami-ku, Hiroshima 734, Japan
      *Corresponding author. Tel: (82) 257 5280; Fax: (82) 257 5284.
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  • Takanori Kumagai,

    1. Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Kasumi 1-2-3, Minami-ku, Hiroshima 734, Japan
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  • Mitsuhiko Shionoya,

    1. Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Kasumi 1-2-3, Minami-ku, Hiroshima 734, Japan
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  • Eiichi Kimura,

    1. Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Kasumi 1-2-3, Minami-ku, Hiroshima 734, Japan
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  • Julian E. Davies

    1. Department of Microbiology, The University of British Columbia, 300-6174 University Boulevard, Vancouver, BC V6T 1Z3, Canada
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*Corresponding author. Tel: (82) 257 5280; Fax: (82) 257 5284.

Abstract

Abstract Bleomycin-producing Streptomyces verticillus ATCC15003 possesses a bleomycin acetyltransferase which inactivates the drug in the presence of acetyl coenzyme A. The site of acylation in enzymically prepared acetylbleomycin A2 was determined by nuclear magnetic resonance analysis; the primary amino group of the β-aminoalanine moiety of bleomycin was acetylated. Acetylbleomycin A2 had no detectable antibacterial activity and did not induce in vitro DNA degradation.

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