DNA interactions of antitumor trans-[PtCl2(NH3)(quinoline)]
| Authors | |
|---|---|
| Year of publication | 1998 |
| Type | Article in Periodical |
| Magazine / Source | EUROPEAN JOURNAL OF BIOCHEMISTRY |
| MU Faculty or unit | |
| Citation | |
| Field | Biochemistry |
| Keywords | DNA; platinum drug; quinoline; antitumor activity; conformation |
| Description | Recent observations that several trans platinum complexes exhibit antitumor activity including activity in cisplatin-resistant tumor cells, violates the classical structure/activity relationships of platinum(II) complexes. According to these relationships, only bifunctional platinum(II) complexes with cis oriented leaving ligands should be therapeutically active. In order to contribute to the understanding of mechanisms underlying the antitumor activity of these new trans platinum analogs, various biochemical and biophysical methods as well as molecular modeling techniques were employed to study the modifications of DNA by antitumor trans[PtCl2(NH3)(quinoline)]. The results indicated that trans[PtCl2(NH3)(quinoline)] coordinated monofunctionally to DNA with a similar rate as transplatin. The overall rate of the rearrange ment to bifunctional adducts was also similar to that observed in the case of DNA modification by transplatin, i.e, it was relatively slow. |