高等学校化学学报

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具有DNA切割功能的新型多聚酰胺/丝组缀合物

牛明玉1; 叶勇2; 刘伟1; 张祯1; 赵玉芬1,2   

  1. 1. 清华大学化学系, 生命有机磷化学及化学生物学教育部重点实验室, 北京 100084;
    2. 郑州大学化学系, 化学生物学和有机化学河南省重点实验室, 郑州 450052
  • 收稿日期:2005-06-07 修回日期:1900-01-01 出版日期:2006-07-10 发布日期:2006-07-10
  • 通讯作者: 赵玉芬

A Novel Polyamide/Ser-His Conjugate with DNA-cleaving Function

NIU Ming-Yu1; YE Yong2; LIU Wei1; ZHANG Zhen1; ZHAO Yu-Fen1,2*   

  1. 1. Key laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology,
    Ministry of Education, Department of Chemistry, Tsinghua University,
    Beijing 100084, China;
    2. Department of Chemistry, Key Laboratory of Chemical Biology and Organic
    Chemistry, Zhengzhou University, Zhengzhou 450052, China
  • Received:2005-06-07 Revised:1900-01-01 Online:2006-07-10 Published:2006-07-10
  • Contact: ZHAO Yu-Fen

摘要: 为得到具有核酸切割功能的人工核酸酶, 设计合成了一种新型多聚酰胺/丝组缀合物, 并研究了其DNA切割活性. 合成的目标化合物在pH=6.0的BR缓冲溶液中对pBR322 DNA切割活性的初步实验结果表明, 于37 ℃保温6 h后, pBR322 DNA基本上被完全从Form Ⅰ切割为Form Ⅱ, 保温36 h后, pBR322 DNA几乎被切割完全.

关键词: 多聚酰胺/丝组缀合物, DNA, 切割试剂

Abstract: Recently, polyamides containing N-methylpyrrole have attracted considerable attention from synthetic and biological chemists. Based on Dervan's theory, the polyamide/SerHis conjugate which is a synthetic analogue of natural products for DNA affinity was synthesized through the dicyclohexylcarbodiimide/1-hydroxybenzotriazole(DCC/HOBt) coupling reaction, and its cleavage activity for DNA was also studied. In BR buffer(pH=60), pBR322 DNA can be cleavaged by the title compound at 37 ℃. After 6 h, pBR 322 DNA was transferred from form Ⅰ to form Ⅱ, after 36 h, pBR 322 DNA was cleavaged totally.

Key words: Polyamide/Ser-His conjugate, DNA, Cleavage agen

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