Structural basis of DNA quadruplex recognition by an acridine drug

被引：277

作者：

Campbell, Nancy H. ^{[1
]}

Parkinson, Gary N. ^{[1
]}

Reszka, Anthony P. ^{[1
]}

Neidle, Stephen ^{[1
]}

机构：

[1] Univ London, Canc Res UK Biomol Struct Grp, Sch Pharm, London WC1N 1AX, England

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2008年 / 130卷 / 21期

关键词：

D O I：

10.1021/ja8016973

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The crystal structure of a complex between the bimolecular human telomeric quadruplex d (TAGGGTTAGGGT)(2) and the experimental anticancer drug BRACO-19, has been determined, to 2.5 angstrom resolution. The binding site for the BRACO-19 molecule is at the interface of two parallel-folded quadruplexes, sandwiched between a G-tetrad surface and a TATA tetrad, and held in the site by networks of water molecules. The structure rationalizes the existing structure-activity data and provides a starting-point for the structure-based design of quadruplex-binding ligands.

引用

页码：6722 / +

页数：4

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