Selectivity in Ligand Recognition of G-Quadruplex Loops

被引：108

作者：

Campbell, Nancy H. ^{[1
]}

Patel, Manisha ^{[1
]}

Tofa, Amina B. ^{[1
]}

Ghosh, Ragina ^{[1
]}

Parkinson, Gary N. ^{[1
]}

Neidle, Stephen ^{[1
]}

机构：

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

来源：

BIOCHEMISTRY | 2009年 / 48卷 / 08期

关键词：

TELOMERIC G-QUADRUPLEX; PROXIMAL PROMOTER; CRYSTAL-STRUCTURE; DRUG RECOGNITION; STRUCTURAL BASIS; SMALL-MOLECULE; DNA; SEQUENCE; TOPOLOGY; STABILITY;

D O I：

10.1021/bi802233v

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of disubstituted acridine ligands have been cocrystallized with a bimolecular DNA G-quadruplex. The ligands have a range of cyclic amino end groups of varying size. The crystal structures show that the diagonal loop in this quadruplex results in a large cavity for these groups, in contrast to the steric constraints imposed by propeller loops in human telomeric quadruplexes. We conclude that the nature of the loop has a significant influence on ligand selectivity for particular quadruplex folds.

引用

页码：1675 / 1680

页数：6

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