CRYSTAL-STRUCTURE OF A PENTAMIDINE OLIGONUCLEOTIDE COMPLEX - IMPLICATIONS FOR DNA-BINDING PROPERTIES

被引：185

作者：

EDWARDS, KJ ^{[1
]}

JENKINS, TC ^{[1
]}

NEIDLE, S ^{[1
]}

机构：

[1] INST CANC RES,CANC RES CAMPAIGN BIOMOLEC STRUCT UNIT,SUTTON SM2 5NG,SURREY,ENGLAND

来源：

BIOCHEMISTRY | 1992年 / 31卷 / 31期

关键词：

D O I：

10.1021/bi00146a011

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：

The crystal structure of the complex formed between the dodecanucleotide d(CGCGAATTCGCG)2 and the drug pentamidine, which is active against the Pneumocystis carinii pathogen in AIDS patients, has been determined to a resolution of 2.1 angstrom and an R-factor of 19.4%. Analysis of the structure has shown the drug to be bound in the 5'-AATT minor groove region of the duplex, with the amidinium groups H-bonded to adenine N3 atoms in an interstrand manner. The drug molecule adopts an extended conformation, and the immediate binding site spans four base pairs. Structural details of the drug-DNA interactions are discussed, and comparison is made with the dodecamer complex of the structurally similar berenil ligand.

引用

页码：7104 / 7109

页数：6

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