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duocarmycin
The duocarmycins are members of a series of related natural products first isolated from ''Streptomyces'' bacteria in 1988.〔(【引用サイトリンク】title=Cytotoxic Agents )〕 They are notable for their extreme cytotoxicity and thus represent a class of exceptionally potent antitumour antibiotics.
==Biological Activity==
As a small-molecule, synthetic, DNA minor groove binding alkylating agents, duocarmycins are suitable to target solid tumors. They bind to the minor groove of DNA and alkylate the nucleobase adenine at the N3 position. The irreversible alkylation of DNA disrupts the nucleic acid architecture, which eventually leads to tumor cell death. Analogues of naturally occurring antitumour agents, such as duocarmycins, represent a new class of highly potent antineoplastic compounds.
The work of Dale L. Boger and others created a better understanding of the pharmacophore and mechanism of action of the duocarmycins. This research has led to synthetic analogs including adozelesin, bizelesin, and carzelesin which progressed into clinical trials for the treatment of cancer.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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