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Publication : Mechanism of action of eukaryotic DNA topoisomerase I and drugs targeted to the enzyme.

First Author  Pommier Y Year  1998
Journal  Biochim Biophys Acta Volume  1400
Issue  1-3 Pages  83-105
PubMed ID  9748515 Mgi Jnum  J:171881
Mgi Id  MGI:5000287 Doi  10.1016/s0167-4781(98)00129-8
Citation  Pommier Y, et al. (1998) Mechanism of action of eukaryotic DNA topoisomerase I and drugs targeted to the enzyme. Biochim Biophys Acta 1400(1-3):83-105
abstractText  DNA topoisomerase I is essential for cellular metabolism and survival. It is also the target of a novel class of anticancer drugs active against previously refractory solid tumors, the camptothecins. The present review describes the topoisomerase I catalytic mechanisms with particular emphasis on the cleavage complex that represents the enzyme's catalytic intermediate and the site of action for camptothecins. Roles of topoisomerase I in DNA replication, transcription and recombination are also reviewed. Because of the importance of topoisomerase I as a chemotherapeutic target, we review the mechanisms of action of camptothecins and the other topoisomerase I inhibitors identified to date.
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