Minor‐groove binders are inhibitors of the catalytic activity of DNA gyrases

FEBS Letters

Störl, K.¹  Störl, J.¹  Lown, J.W.²  Zimmer, Ch.¹ 

[1] Department of Molecular Biology, Institute of Molecular Biology, University of Jena, Jena, Germany;Department of Chemistry, University of Alberta, Edmonton, AB, Canada

关键词: DNA binding drug;    Inhibition;    DNA gyrase;    Streptomyces noursei;    Dst-3;    distamycin A;    Nt=Nt-PyPy;    netropsin containing methylpyrrole (Py);    Nt-Pylm;    Nt-ImPy;    Nt-Im3;    netropsin analogs (lexitropsins) containing methylimidazole (Im) and (or) methylpyrrole (Py);    bis-Nt-X (X = 5;    6;    8);    dimeric netropsin analogs linked by X methyleneresidues(X=5;    6;    8);    DAPI;    4';    6-di-amidino-phenylindole;    Hoechst 33258;    2-(4-hydroxyphenyl)-5-[5-(4-methyl-piperazin-1-yl)-benzimidazole-2-yl]benzimidazole;    SN-6999;    NSC-101327;    SN-6132;    SN-6131;    SN-16814;    SN-1871;    bisquaternary ammonium heterocycles (structures are given in [10;    22]);    SDS;    sodium dodecylsulfate;   

DOI  :  10.1016/0014-5793(93)81513-Y

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Non-intercalating DNA minor-groove binders may effectively inhibit the supercoiling activity of gyrases by influencing the enzyme recognition and cleavage site on DNA. For gyrase from Streptomyces noursei a wide range of inhibitory potency for different classes of ligands is observed. This can be explained by a number of structural and binding factors of the ligands competing with the gyrase on the target site of DNA, the mechanism of which is different from the classical gyrase inhibitors.

【 授权许可】

Unknown