Abstract

Biosynthetic intermediates and synthetic analogues of bleomycin ( BLM) have been investigated for their metal binding, dioxygen activation, and DNA cleavage. Molecular O 2 was activated by the Fe(II) complex of a synthetic model ligand. Nucleotide sequence specificities in DNA cleavage by the BLM-Fe(II) and deglyco- BLM-Fe(II) complexes were almost identical. It has been shown that (1) the β-aminoalanine-pyrimidine-β-hydroxyhistidine portion of BLM is essential for the metal binding and dioxygen activation and (2) the bithiazole moiety contributes to the specific binding to guanine base of DNA.

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