publication . Article . 2006

Topoisomerase I inhibitors: camptothecins and beyond

Pommier, Yves;
Open Access
  • Published: 01 Oct 2006
  • Publisher: Springer Science and Business Media LLC
Abstract
Topoisomerase I (TOP1) enzymes are essential in higher eukaryotes, as they are required to relax DNA supercoiling generated by transcription, replication and chromatin remodelling. Topoisomerases are particularly vulnerable to topoisomerase I inhibitors during their cleavage reaction, which is referred to as the 'cleavage complex'. TOP1 can be trapped by anticancer drugs as it cleaves DNA. Moreover, TOP1 can be trapped by endogenous alterations to DNA (mismatches, abasic sites, nicks and adducts) and apoptotic alterations to chromatin. Camptothecin is a natural product of which TOP1 is the only cellular target. Two camptothecin derivatives have recently been app...
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free text keywords: Biochemistry, Topotecan, medicine.drug, medicine, Biology, Topoisomerase, biology.protein, Topoisomerase-I Inhibitor, TDP1, DNA damage, Irinotecan, DNA repair, Camptothecin
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