Skip Navigation

This Article
Right arrow Print PDF (3234K)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrow Search for citing articles in:
ISI Web of Science (82)
Right arrowRequest Permissions
Right arrow Commercial Re-use Guidelines
for Open Access NAR Content
Google Scholar
Right arrow Articles by Pommier, Y.
Right arrow Articles by Pham, R.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Pommier, Y.
Right arrow Articles by Pham, R.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

Nucleic Acids Research, 1987, Vol. 15, No. 16 6713-6731
© 1987

Articles

DNA unwinding and inhibition of mouse leukemia L1210 DNA topoisomerase I by intercalators

Yves Pommier, Joseph M. Covey, Donna Kerrigan, Judith Markovits and Richard Pham

Laboratory of Molecular Pharmacology, Division of Cancer Treatment, National Cancer Institute National Institutes of Health, Bethesda, MD 20892, USA

Received April 28, 1987. Revised July 10, 1987. Accepted July 10, 1987.

The DNA unwinding effects of some 9-aminoacridine derivatives were compared under reaction conditions that could be used to study drug-induced topoisomerase II inhibition. An assay was designed to determine drug-induced DNA unwinding by using L1210 topoisomerase I. 9-aminoacridines could be ranked by decreasing unwinding potency: compound C > 9-aminoacridine > o-AMSA > compound A > compound B > m-AMSA. Ethidium bromide was more potent than any of the 9-aminoacridines. This assay is a fast and simple method to compare DNA unwinding effects of intercalators. It led to the definition of a drug intrinsic unwinding constant (k). An additional finding was that all 9-aminoacridines and ethidium bromide inhibited L1210 topoisomerase I. Enzyme inhibiton was detectable at low enzyme concentrations (< 1 unit) and when the kinetics of topoisomerase I-mediated DNA relaxation was studied. Topoisomerase I inhibition was not associated with DNA swivelling or cleavage.


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 Nucleic Acids ResHome page
C. Marchand, K. Krajewski, H.-F. Lee, S. Antony, A. A. Johnson, R. Amin, P. Roller, M. Kvaratskhelia, and Y. Pommier
Covalent binding of the natural antimicrobial peptide indolicidin to DNA abasic sites
Nucleic Acids Res., October 6, 2006; (2006) gkl667v3.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
S. Antony, K. K. Agama, Z.-H. Miao, M. Hollingshead, S. L. Holbeck, M. H. Wright, L. Varticovski, M. Nagarajan, A. Morrell, M. Cushman, et al.
Bisindenoisoquinoline Bis-1,3-{(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA Intercalator and Topoisomerase Inhibitor with Antitumor Activity
Mol. Pharmacol., September 1, 2006; 70(3): 1109 - 1120.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
K. Umemura, T. Mizushima, H. Katayama, Y. Kiryu, T. Yamori, and T. Andoh
Inhibition of DNA Topoisomerases II and/or I by Pyrazolo[1,5-a]indole Derivatives and Their Growth Inhibitory Activities
Mol. Pharmacol., October 1, 2002; 62(4): 873 - 880.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
W. Nieves-Neira, M. I. Rivera, G. Kohlhagen, M. L. Hursey, P. Pourquier, E. A. Sausville, and Y. Pommier
DNA Protein Cross-Links Produced by NSC 652287, a Novel Thiophene Derivative Active Against Human Renal Cancer Cells
Mol. Pharmacol., September 1, 1999; 56(3): 478 - 484.
[Abstract] [Full Text]

Home page
 Cancer Res.Home page
C. Bailly, L. Dassonneville, P. Colson, C. Houssier, K. Fukasawa, S. Nishimura, and T. Yoshinari
Intercalation into DNA Is Not Required for Inhibition of Topoisomerase I by Indolocarbazole Antitumor Agents
Cancer Res., June 1, 1999; 59(12): 2853 - 2860.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
G. Kohlhagen, K. D. Paull, M. Cushman, P. Nagafuji, and Y. Pommier
Protein-Linked DNA Strand Breaks Induced by NSC 314622, a Novel Noncamptothecin Topoisomerase I Poison
Mol. Pharmacol., July 1, 1998; 54(1): 50 - 58.
[Abstract] [Full Text]


Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.