Mechanism of bleomycin action: In vitro studies

Richard M. Burger; Jack Peisach; Susan Band Horwitz

doi:10.1016/0024-3205(81)90153-3

Mechanism of bleomycin action: In vitro studies

Richard M. Burger, Jack Peisach, Susan Band Horwitz

Molecular Pharmacology

Research output: Contribution to journal › Article › peer-review

127 Scopus citations

Abstract

The cytotoxic activity of bleomucin results from DNA cleavage, which is also accomplished in vitro by reaction mixtures containing Fe(II), drug and O₂. Bleomycin forms a complex with Fe(II) and O₂ in the presence or absence of DNA. The species attacking DNA forms rapidly from this complex. The nature of the attacking species and of the primary lesion(s) to DNA are not yet known, but two major insults to DNA have been characterized. They are the release of free bases from their glycosidic linkages and, at other residues, the cleavage of the polymer backbone at the deoxyribose C3-C4 bond.

Original language	English (US)
Pages (from-to)	715-727
Number of pages	13
Journal	Life Sciences
Volume	28
Issue number	7
DOIs	https://doi.org/10.1016/0024-3205(81)90153-3
State	Published - Feb 16 1981

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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abstract = "The cytotoxic activity of bleomucin results from DNA cleavage, which is also accomplished in vitro by reaction mixtures containing Fe(II), drug and O2. Bleomycin forms a complex with Fe(II) and O2 in the presence or absence of DNA. The species attacking DNA forms rapidly from this complex. The nature of the attacking species and of the primary lesion(s) to DNA are not yet known, but two major insults to DNA have been characterized. They are the release of free bases from their glycosidic linkages and, at other residues, the cleavage of the polymer backbone at the deoxyribose C3-C4 bond.",

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AB - The cytotoxic activity of bleomucin results from DNA cleavage, which is also accomplished in vitro by reaction mixtures containing Fe(II), drug and O2. Bleomycin forms a complex with Fe(II) and O2 in the presence or absence of DNA. The species attacking DNA forms rapidly from this complex. The nature of the attacking species and of the primary lesion(s) to DNA are not yet known, but two major insults to DNA have been characterized. They are the release of free bases from their glycosidic linkages and, at other residues, the cleavage of the polymer backbone at the deoxyribose C3-C4 bond.

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Mechanism of bleomycin action: In vitro studies

Abstract

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