Affordable Access

deepdyve-link deepdyve-link
Publisher Website

Etoposide catechol is an oxidizable topoisomerase II poison.

Authors
  • Jacob, David A
  • Gibson, Elizabeth G
  • Mercer, Susan L
  • Deweese, Joseph E
Type
Published Article
Journal
Chemical Research in Toxicology
Publisher
American Chemical Society
Publication Date
Aug 19, 2013
Volume
26
Issue
8
Pages
1156–1158
Identifiers
DOI: 10.1021/tx400205n
PMID: 23863110
Source
Medline
License
Unknown

Abstract

Topoisomerase II regulates DNA topology by generating transient double-stranded breaks. The anticancer drug etoposide targets topoisomerase II and is associated with the formation of secondary leukemias in patients. The quinone and catechol metabolites of etoposide may contribute to strand breaks that trigger leukemic translocations. To further analyze the characteristics of etoposide metabolites, we extend our previous analysis of etoposide quinone to the catechol. We demonstrate that the catechol is ∼2-3-fold more potent than etoposide and under oxidative reaction conditions induces high levels of double-stranded DNA cleavage. These results support a role for etoposide catechol in contributing to therapy-induced DNA damage.

Report this publication

Statistics

Seen <100 times