DNAの認識と切断 : 機能性インターカレーターの分子設計

概要

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Bis-intercalators and hemin-intercalators (Hemin-Glu-P-1s) which recognize and/or cleave DNA were designed and synthesized. 2-Aminodipyrido [1, 2-a : 3, 2 -d] imidazoles (Glu-Ps) which are potent muta-carcinogens isolated from a pyrolysate of L-glutamic acid were used as intercalator moieties. Bis-intercalators possess extremely high affinity toward double stranded DNA and stabilize the double helix structure of DNA from heat denaturation effectively. Hemin-Glu-P-1s cleaved DNA at G-C and G-T sequences preferentially. Glu-P-1 moiety which recognizes DNA by intercalation and a functional group which can be an intramolecular fifth ligand of the ferrous ion in the hemin moiety are required for strong DNA-cleaving ability. The mode of DNA-cleaving reaction of Hemin-Glu-P-1s is quite similar to that of bleomycin (BLM). In other words, Hemin-Glu-P-1s are functional analogs of BLM. The mechanism of DNA cleavage by Hemin-Glu-P-1s and by BLM is not single. One of the mechanisms involves two bases elimination from the DNA.
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