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O6-甲基鸟嘌呤-DNA甲基转移酶对DNA中O6-甲基鸟嘌呤的去甲基化作用:N7位与顺铂配位的O6,9-二甲基鸟嘌呤的合成与表征。

Demethylation of O6-methylguanine in DNA by O6-methylguanine-DNA methyltransferase: synthesis and characterization of O6,9-dimethylguanine coordinated with cis-platin at the N7-position.

作者信息

Terashima I, Yamagata Y, Yamagami N, Kohda K

机构信息

Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1994 Apr;42(4):903-6. doi: 10.1248/cpb.42.903.

Abstract

In order to investigate the chemical characteristics of O6-methylguanines, the substrate of O6-methylguanine-DNA methyltransferase, cis[PtCl(NH3)2(O6,9-dimethylguanine-7)]NO3, a 1:1 complex of cis-platin with O6,9-dimethylguanine, was synthesized and its demethylation rate, pKa, X-ray structure and cytotoxicity were determined.

摘要

为了研究O6-甲基鸟嘌呤-DNA甲基转移酶的底物O6-甲基鸟嘌呤的化学特性,合成了顺式[PtCl(NH3)2(O6,9-二甲基鸟嘌呤-7)]NO3,即顺铂与O6,9-二甲基鸟嘌呤的1:1配合物,并测定了其去甲基化速率、pKa、X射线结构和细胞毒性。

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