Oncologie

, Volume 9, Issue 11, pp 758–765 | Cite as

Les poisons des topo-isomérases I

Oncologie Pharmacologie
First Online:

Résumé

Les enzymes topo-isomérases I interviennent pour résoudre des contraintes topologiques de l’ADN. Les topo-isomérases I coupent transitoirement un seul des deux brins d’ADN et transfèrent l’autre brin au travers de la coupure transitoire, avant de relier. Les poisons de topo-isomérase I en clinique sont les dérivés de la camptothécine: irinotécan ou 7-éthyl-10-[4-(I-pipéridino)-I-pipéridino]carbonyloxy-camptothécine (Campto®), topotécan ou 9-(diméthylamino)méthyl-10-hydroxycampto-thécine (Hycamtin®). Les principales propriétés pharmacologiques et cliniques des dérivés de camptothécine sont revues.

Mots clés

Topo-isomérases Irinotécan Topotécan Pharmacologie 

Topo-isomerase I inhibitors

Abstract

Topo-isomerase I is involved in resolving topological constraints in DNA. It transiently cleaves one of the two strands of DNA, passes the other through the transient break, and then ligates the break. The topo-isomerase I inhibitors used in clinical practice are camptothecin derivatives: irinotecan (7-ethyl-10-[4-(I-piperidino)-I-piperidino]carbonyloxy-camptothecine [Campto®]) and topotecan (9-(dimethylamino)methyl-10-hydroxycamptothecine [Hycamtin®]). We review the main pharmacological and clinical properties of the camptothecin derivatives.

Keywords

Topo-isomerase Irinotecan Topotecan Pharmacology 
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Copyright information

© Springer Verlag France 2007

Authors and Affiliations

  1. 1.Unité de cancérologie médicalehôpital CochinParisFrance

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