[Topoisomerases: therapeutic value].

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Faure P, Madelaine I

[Topoisomerases: therapeutic value].

Ann Pharm Fr. 1996;54(1):40-4.

PubMed ID

8702194 [ View in PubMed

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Abstract

Anticancer pharmacology offers rich prospects for future therapeutic design. Knowledge of antitumoral agents pharmacology have widely advanced: understanding of the molecular cytotoxic mechanism of available agents, discovery of new compounds with a different and no-interfering mechanism of action. Since ten years, the identification of a couple of nuclear enzyme, DNA-topoisomerases, has answered to this goal. These enzymes catalyse the topological changes of the double strand DNA, participating to vital processes of cell metabolism. These enzymes are now know to be the intracellular target of widely used cytotoxic agents (such as anthracycline, Etoposide, Teniposide for DNA topoisomerase II) and for two new compounds in clinical trials (irinotecan and topotecan, both analogues of camptothecin, for DNA-topoisomerase I). This two last molecules, currently in phase II development, are promising. They seem to be synergistic in combination with available anticancer agents, but this remains to be demonstrated. Other drugs, inhibiting both DNA-topoisomerases I and II, are yet investigating. Would they provide new answers for the future?

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Teniposide	DNA topoisomerase 2-alpha	Protein	Humans	Yes	Inhibitor	Details