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Inactivation of bleomycin by an N-acetyltransferase in the bleomycin-producing strain Streptomyces verticillus |
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| Authors: | Masanori Sugiyama Takanori Kumagai Mitsuhiko Shionoya Eiichi Kimura Julian E. Davies |
| Affiliation: | Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Kasumi 1-2-3, Minami-ku, Hiroshima 734, Japan; Department of Microbiology, The University of British Columbia, 300-6174 University Boulevard, Vancouver, BC V6T 1Z3, Canada |
| 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. |
| Keywords: | N-Acetylbleomycin Bleomycin N-acetyltransferase Proton nuclear magnetic resonance Self-resistance Streptomyces verticillus |