Inactivation of bleomycin by an N-acetyltransferase in the bleomycin-producing strain Streptomyces verticillus.
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 beta-aminoalanine moiety of bleomycin was acetylated Acetylbleomycin A2 had no detectable antibacterial activity and did not induce in vitro DNA degradation.
Sugiyama
M
M
Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Japan.
Kumagai
T
T
Shionoya
M
M
Kimura
E
E
Davies
J E
JE
D000123:Acetyltransferases / Q000378:metabolism*; D001761:Bleomycin / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology* / Q000031:analogs & derivatives; D009682:Magnetic Resonance Spectroscopy; D013302:Streptomyces / Q000378:metabolism*
C026658:acetylbleomycin A2; D001761:Bleomycin; D000123:Acetyltransferases