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一种用于合成柔性环状聚酰胺的便捷方法,用于选择性靶向 c-myb G-四链体 DNA。

Convenient method for the synthesis of a flexible cyclic polyamide for selective targeting of c-myb G-quadruplex DNA.

机构信息

Beijing National Laboratory for Molecular Sciences, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.

出版信息

Org Lett. 2012 Dec 21;14(24):6126-9. doi: 10.1021/ol302918f. Epub 2012 Dec 4.

Abstract

A convenient efficient method for synthesis of a flexible cyclic polyamide (cβ, 1) was developed through cyclodimerization. Electrospray ionization mass spectrometry and nuclear magnetic resonance results showed that 1 selectively binds to the c-myb G-quadruplex with high affinity, and there was no binding with the ILPR, bcl-2, and c-kit G-quadruplexes. This is the first time that a flexible cyclic polyamide was found to have high selectivity for the c-myb G-quadruplex.

摘要

通过环二聚化,开发了一种方便高效的合成柔性环聚酰胺(cβ,1)的方法。电喷雾电离质谱和核磁共振结果表明,1 选择性地与 c-myb G-四链体高亲和力结合,与 ILPR、bcl-2 和 c-kit G-四链体没有结合。这是首次发现柔性环聚酰胺对 c-myb G-四链体具有高选择性。

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