Inhibition of human topoisomerase II by the antitumor metallocenes

G. Mokdsi; M. M. Harding

doi:10.1016/S0162-0134(00)00198-7

Inhibition of human topoisomerase II by the antitumor metallocenes

G. Mokdsi, M. M. Harding^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

86 Citations (Scopus)

Abstract

The ability of antitumor active metallocenes Cp₂MCl₂, (M=Ti, V, Mo, Nb) and the biologically inactive derivative (MeCp)₂TiCl₂, to inhibit the relaxation of supercoiled plasmid DNA pBR322 by human topoisomerase II has been studied by gel electrophoresis. All metallocenes inhibit the enzyme with maximum 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 discussed.

Original language	English
Pages (from-to)	205-209
Number of pages	5
Journal	Journal of Inorganic Biochemistry
Volume	83
Issue number	2-3
DOIs	https://doi.org/10.1016/S0162-0134(00)00198-7
Publication status	Published - 15 Jan 2001
Externally published	Yes

Access to Document

10.1016/S0162-0134(00)00198-7

Cite this

@article{a15e4b1849ce45d49bb91405670a5969,

title = "Inhibition of human topoisomerase II by the antitumor metallocenes",

abstract = "The ability of antitumor active metallocenes Cp2MCl2, (M=Ti, V, Mo, Nb) and the biologically inactive derivative (MeCp)2TiCl2, to inhibit the relaxation of supercoiled plasmid DNA pBR322 by human topoisomerase II has been studied by gel electrophoresis. All metallocenes inhibit the enzyme with maximum 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 discussed.",

keywords = "Antitumor, DNA relaxation, Metallocene dihalides, Topoisomerase II, Topoisomerase inhibition",

author = "G. Mokdsi and Harding, {M. M.}",

year = "2001",

month = jan,

day = "15",

doi = "10.1016/S0162-0134(00)00198-7",

language = "English",

volume = "83",

pages = "205--209",

journal = "Journal of Inorganic Biochemistry",

issn = "0162-0134",

publisher = "Elsevier Inc.",

number = "2-3",

}

TY - JOUR

T1 - Inhibition of human topoisomerase II by the antitumor metallocenes

AU - Mokdsi, G.

AU - Harding, M. M.

PY - 2001/1/15

Y1 - 2001/1/15

N2 - The ability of antitumor active metallocenes Cp2MCl2, (M=Ti, V, Mo, Nb) and the biologically inactive derivative (MeCp)2TiCl2, to inhibit the relaxation of supercoiled plasmid DNA pBR322 by human topoisomerase II has been studied by gel electrophoresis. All metallocenes inhibit the enzyme with maximum 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 discussed.

AB - The ability of antitumor active metallocenes Cp2MCl2, (M=Ti, V, Mo, Nb) and the biologically inactive derivative (MeCp)2TiCl2, to inhibit the relaxation of supercoiled plasmid DNA pBR322 by human topoisomerase II has been studied by gel electrophoresis. All metallocenes inhibit the enzyme with maximum 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 discussed.

KW - Antitumor

KW - DNA relaxation

KW - Metallocene dihalides

KW - Topoisomerase II

KW - Topoisomerase inhibition

UR - http://www.scopus.com/inward/record.url?scp=0035863121&partnerID=8YFLogxK

U2 - 10.1016/S0162-0134(00)00198-7

DO - 10.1016/S0162-0134(00)00198-7

M3 - Article

SN - 0162-0134

VL - 83

SP - 205

EP - 209

JO - Journal of Inorganic Biochemistry

JF - Journal of Inorganic Biochemistry

IS - 2-3

ER -

Inhibition of human topoisomerase II by the antitumor metallocenes

Abstract

Access to Document

Other files and links

Fingerprint

Cite this