Ueyama H, Waki M, Takagi M, Takenaka S
Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, Fukuoka 812-8581, Japan.
Nucleic Acids Symp Ser. 2000(44):133-4. doi: 10.1093/nass/44.1.133.
Tetra-acridinyl peptide 2 was synthesized from Fmoc-Lys(Boc)-OH and Fmoc-Lys(Acr)-OH (1) with the peptide synthesizer. The CD measurement suggested that 2 forms a special organized structure by itself in buffered solution. Peptide 2 binds to double stranded DNA with a very large affinity constant, which is 10(3)-times larger than that of quinacrine. Spectrophotometric and hydrodynamic studies suggested that all of the acridinyl parts of 2 contribute to the intercalating interaction for the DNA binding. Our finding in this experiment demonstrates that polyintercalators such as 2 can be assembled quickly by the automated synthesizer.
四吖啶基肽2由Fmoc-Lys(Boc)-OH和Fmoc-Lys(Acr)-OH(1)通过肽合成仪合成。圆二色性测量表明，2在缓冲溶液中自身形成一种特殊的有序结构。肽2以非常大的亲和常数与双链DNA结合，该常数比喹吖因的亲和常数大10³倍。分光光度法和流体动力学研究表明，2的所有吖啶基部分都有助于与DNA结合的嵌入相互作用。我们在本实验中的发现表明，像2这样的多嵌入剂可以通过自动合成仪快速组装。
