Oxazole-based peptide macrocycles: A new class of G-quadruplex binding ligands

被引：112

作者：

Jantos, Katja ^{[1
]}

Rodriguez, Raphael ^{[1
]}

Ladame, Sylvain ^{[1
]}

Shirude, Pravin S. ^{[1
]}

Balasubramanian, Shankar ^{[1
]}

机构：

[1] Univ Cambridge, Univ Chem Lab, Cambridge CB2 1EW, England

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2006年 / 128卷 / 42期

关键词：

D O I：

10.1021/ja064713e

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Herein we report on the synthesis and DNA binding properties of a new class of water soluble oxazole-based peptide macrocycles that bind selectively to quadruplex DNA, with no detectable binding to duplex DNA. We have recently identified one quadruplex in the proto-oncogene c-kit that is suspected to act as a regulatory element for the expression of the c-kit gene. Here we provide the first example of a ligand binding to and stabilizing the c-kit quadruplex. Moreover, we show that these macrocycles show a preference for the c-kit quadruplex as compared to the human telomeric quadruplex. Copyright © 2006 American Chemical Society.

引用

页码：13662 / 13663

页数：2

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