Inhibition of human topoisomerase II by the antitumor metallocenes

Authors
Mokdsi, G Harding, MM
Citation
G. Mokdsi et Mm. Harding, Inhibition of human topoisomerase II by the antitumor metallocenes, J INORG BIO, 83(2-3), 2001, pp. 205-209
Citations number
33
Categorie Soggetti
Biochemistry & Biophysics","Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF INORGANIC BIOCHEMISTRY
ISSN journal
01620134 → ACNP
Volume
83
Issue
2-3
Year of publication
2001
Pages
205 - 209
Database
ISI
SICI code
0162-0134(20010115)83:2-3<205:IOHTIB>2.0.ZU;2-R
Abstract
The ability of antitumor active metallocenes Cp2MCl2, (M = Ti, V, Mo, Nb) a nd the biologically inactive derivative (MeCp)(2)TiCl2, to inhibit the rela xation of supercoiled plasmid DNA pBR322 by human topoisomerase II has been studied by gel electrophoresis. All metallocenes inhibit the enzyme with m aximum inhibition observed at 2.0 mM (Cp2TiCl2), 3.0 mM (Cp2MoCl2), 0.2 mM (Cp2NbCl2), 0.25 mM (Cp2VCl2) and 2.0 mM (MeCpTiCl2). The implications for the mechanism of antitumor activity of the metallocene dihalides are discus sed. (C) 2001 Elsevier Science B.V. All rights reserved.