A DNA polymerase stop assay for G-quadruplex-interactive compounds

被引：220

作者：

Han, HY

Hurley, LH

Salazar, M ^{[1
]}

机构：

[1] Univ Texas, Coll Pharm, Div Med Chem, Austin, TX 78712 USA

[2] Univ Texas, Coll Pharm, Program Mol Biol, Austin, TX 78712 USA

[3] Univ Texas, Coll Pharm, Drug Dynam Inst, Austin, TX 78712 USA

来源：

NUCLEIC ACIDS RESEARCH | 1999年 / 27卷 / 02期

关键词：

D O I：

10.1093/nar/27.2.537

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：

We have developed and characterized an assay for G-quadruplex-interactive compounds that makes use of the fact that G-rich DNA templates present obstacles to DNA synthesis by DNA polymerases. Using Tao DNA polymerase and the G-quadruplex binding 2,6-diamidoanthraquinone BSU-1051, we find that BSU-1051 leads to enhanced arrest of DNA synthesis in the presence of K+ by stabilizing an intramolecular G-quadruplex structure formed by four repeats of either TTGGGG or TTAGGG in the template strand. The data provide additional evidence that BSU-1051 modulates telomerase activity by stabilization of telomeric G-quadruplex DNA and point to a polymerase arrest assay as a sensitive method for screening for G-quadruplex-interactive agents with potential clinical utility.

引用

页码：537 / 542

页数：6

共 33 条

[1] ANTHRACENE-9,10-DIONES AS POTENTIAL ANTICANCER AGENTS - SYNTHESIS, DNA-BINDING, AND BIOLOGICAL STUDIES ON A SERIES OF 2,6-DISUBSTITUTED DERIVATIVES [J].