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    • 1. 发明授权
    • Method of the solid phase synthesis of pyrrole-imidazole polyamide
    • 吡唑咪唑聚酰胺的固相合成方法
    • US07067622B2
    • 2006-06-27
    • US10481275
    • 2002-02-27
    • Hiroshi SugiyamaHirokazu IidaIsao SaitoTakashi Saito
    • Hiroshi SugiyamaHirokazu IidaIsao SaitoTakashi Saito
    • C07K1/02
    • C07D403/14
    • It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.
    • 本发明提供一种制备吡咯 - 咪唑聚酰胺的方法,其中可以方便地合成较长的吡咯 - 咪唑聚酰胺,并且可以容易地转移肽(蛋白质)。 根据该方法,可以在其末端从固相载体上切割出具有羧酸酯基的吡咯 - 咪唑聚酰胺,从而可以直接转移各种官能团,并且能够精确地区分DNA序列。 一种合成吡咯 - 咪唑聚酰胺的方法,其特征在于使用肽合成仪通过固相Fmoc法进行自动合成; 通过该方法得到的具有羧基的吡咯 - 咪唑聚酰胺; 具有在上述吡咯 - 咪唑聚酰胺末端转移到羧基中的DNA烷基化剂的吡咯 - 咪唑聚酰胺; 特征在于使用上述化合物的序列特异性DNA烷基化方法。