Skip Navigation

This Article
Right arrow Print PDF (555K)
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 (63)
Right arrowRequest Permissions
Right arrow Commercial Re-use Guidelines
for Open Access NAR Content
Google Scholar
Right arrow Articles by Hénichart, J.-P.
Right arrow Articles by Houssin, R.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Hénichart, J.-P.
Right arrow Articles by Houssin, R.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

Nucleic Acids Research, 1985, Vol. 13, No. 18 6703-6717
© 1985

Articles

Is the bithiazole moiety of bleomycin a classical intercalator?

Jean-Pierre Hénichart, Jean-Luc Bernier, Nicole Helbecque1 and Raymond Houssin2

INSERM U 16 Place de Verdun 1Département de Biochimie, Faculté de Médecine, Place de Verdun 2Laboratoire de Chimie de Synthèse des Médicaments, Faculté de Pharmacie, rue Laguesse 59045 Lille, France

Received July 8, 1985. Revised September 6, 1985. Accepted September 6, 1985.

Bleomycin is a widespread anticancerous drug, the biological activity of which having been extensively studied. Its metal ion-chelat1ng portion has been shown to cleave DNA whereas the role of the bithiazole moiety is still questionable. In order to elucidate this problem some 2',4-disubstituted bithiazoles structurally related to the "tripeptide S" moiety of bleomycin were synthesized and their interaction with DNA was studied using 4Tm, fluorescence, EPR and viscometry techniques. The results of 4Tm and fluorescence quenching determinations were in favour of a binding of the bithiazole part by an intercalation process. Nevertheless, the use of the spin-label probes indicated only a partial intercalation of the ring between the base-pairs. Moreover, viscometry data which clearly exhibited a slight decrease of DNA length in the presence of bithiazole derivative led to the proposal of a binding model involving a partial insertion of a thiazole ring which wedges in between the bases at a bending point of DNA.


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




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.