l-Histidyl-glycyl-glycyl-l-histidine. Amino-acid structuring of the bleomycin-type pentadentate metal-binding environment capable of efficient double-strand cleavage of plasmid DNA

• A tetrapeptide, l-histidyl-glycyl-glycyl-l-histidine (HGGH), was synthesized.
• The pUC19 plasmid DNA cleaving activity of Cu(II)−HGGH was investigated.
• Cu(II)−HGGH (50 nM) converted a supercoiled DNA efficiently to a linear DNA.
• The DNA cleavage took place in the presence of 500 μM H2O2/sodium ascorbate.

A tetrapeptide, l-histidyl-glycyl-glycyl-l-histidine (HGGH), was synthesized and the pUC19 plasmid DNA cleaving activity by copper(II) complex of HGGH (Cu(II)−HGGH) was investigated. Cu(II)−HGGH showed bleomycin-like DNA cleaving activity and, at 50 nM, converted a supercoiled DNA efficiently to a linear DNA in the presence of 500 μM H2O2/sodium ascorbate through an oxidative pathway.

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