CaltechAUTHORS
  A Caltech Library Service

Selective inhibition of DNA gyrase in vitro by a GC specific eight-ring hairpin polyamide at nanomolar concentration

Simon, H. and Kittler, L. and Baird, E. and Dervan, P. and Zimmer, C. (2000) Selective inhibition of DNA gyrase in vitro by a GC specific eight-ring hairpin polyamide at nanomolar concentration. FEBS Letters, 471 (2-3). pp. 173-176. ISSN 0014-5793 . http://resolver.caltech.edu/CaltechAUTHORS:20160510-091111559

Full text is not posted in this repository. Consult Related URLs below.

Use this Persistent URL to link to this item: http://resolver.caltech.edu/CaltechAUTHORS:20160510-091111559

Abstract

The influence of an eight-ring hairpin DNA minor groove binder on the gyrase mediated DNA supercoiling and cleavage reaction step of the enzyme was investigated. The results demonstrate that supercoiling is affected by the hairpin polyamide in the millimolar concentration range while the enzyme catalyzed cleavage of a 162 bp fragment of pBR322 containing a single strong gyrase site is effectively inhibited at nanomolar concentration. As demonstrated by footprint analysis the latter effect is caused by a specific binding of the hairpin forming polyamide to the enzyme recognition site (GGCC), which indicates that the gyrase activity to produce a double strand break is blocked at this site. The pyrrole-imidazole hairpin polyamide is the most potent inhibitor of the gyrase mediated cleavage reaction compared to other known anti-gyrase active DNA binding agents.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1016/S0014-5793(00)01390-9DOIArticle
http://onlinelibrary.wiley.com/doi/10.1016/S0014-5793(00)01390-9/abstractPublisherArticle
Additional Information:© 2000 Federation of European Biochemical Societies. Received 2 March 2000. The support of this work by Thüringer Ministerium für Wissenschaft und Kultur is gratefully acknowledged.
Funders:
Funding AgencyGrant Number
Thüringer Ministerium für Wissenschaft und KulturUNSPECIFIED
Subject Keywords:DNA gyrase; Inhibition; Minor groove binder
Record Number:CaltechAUTHORS:20160510-091111559
Persistent URL:http://resolver.caltech.edu/CaltechAUTHORS:20160510-091111559
Official Citation:Simon H.,Kittler L.,Baird E.,Dervan P. and Zimmer C.(2000), Selective inhibition of DNA gyrase in vitro by a GC specific eight-ring hairpin polyamide at nanomolar concentration, FEBS Letters, 471, doi: 10.1016/S0014-5793(00)01390-9
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:66849
Collection:CaltechAUTHORS
Deposited By: Victoria Brennan
Deposited On:18 May 2016 19:35
Last Modified:18 May 2016 19:35

Repository Staff Only: item control page