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Molecular Pharmacology, Vol 16, 256-260, Copyright © 1979 by the American Society for Pharmacology and Experimental Therapeutics

Bleomycin A2: A Ferrous Oxidase

WILLIAM J. CASPARY 1, CRAIG NIZIAK 1, D. ALLAN LANZO 1, ROSALIND FRIEDMAN 1, and NICHOLAS R. BACHUR 1

1 Laboratory of Clinical Biochemistry, Baltimore Cancer Research Program, National Cancer Institute, National Institutes of Health, 655 W. Baltimore St., Baltimore, Maryland 21201

The bleomycins are polypeptides produced by Streptomyces verticullus and are used in chemotherapy of various malignancies. We find that bleomycin A2 catalyzes the oxidation of Fe++ to Fe+++ and reduces oxygen. The reaction follows classical Michaelis-Menten kinetics (Vmax = 0.27 µmole/min/ml, Km = 1.8 mM). One mole of bleomycin A2 turns over approximately 5,000 moles Fe++/min. This catalytic activity of bleomycin A2 is heat insensitive and strongly dependent on pH, buffer and ionic strength, and is unaffected by DNA. This enzyme-like action may be involved in the bleomycin degradation of DNA.

Submitted on September 21, 1978
Accepted on January 19, 1979






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