Substitution-Inert Polynuclear Platinum Complexes with Dangling Amines: Condensation/Aggregation of Nucleic Acids and Inhibition of DNA-Related Enzymatic Activities
Language English Country United States Media print-electronic
Document type Journal Article
- MeSH
- Amines chemistry MeSH
- DNA Topoisomerases, Type I drug effects MeSH
- DNA chemistry MeSH
- Topoisomerase I Inhibitors MeSH
- Coordination Complexes chemistry MeSH
- Microscopy, Atomic Force MeSH
- Antineoplastic Agents chemistry MeSH
- RNA chemistry MeSH
- Platinum Compounds chemistry MeSH
- Taq Polymerase antagonists & inhibitors MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Amines MeSH
- DNA Topoisomerases, Type I MeSH
- DNA MeSH
- Topoisomerase I Inhibitors MeSH
- Coordination Complexes MeSH
- Antineoplastic Agents MeSH
- RNA MeSH
- Platinum Compounds MeSH
- Taq Polymerase MeSH
The substitution-inert polynuclear platinum complexes (SI-PPCs) are now recognized as a distinct subclass of platinum anticancer drugs with high DNA binding affinity. Here, we investigate the effects of SI-PPCs containing dangling amine groups in place of NH3 as ligands to increase the length of the molecule and therefore overall charge and its distribution. The results obtained with the aid of biophysical techniques, such as total intensity light scattering, gel electrophoresis, and atomic force microscopy, show that addition of dangling amine groups considerably augments the ability of SI-PPCs to condense/aggregate nucleic acids. Moreover, this enhanced capability of SI-PPCs correlates with their heightened efficiency to inhibit DNA-related enzymatic activities, such as those connected with DNA transcription, catalysis of DNA relaxation by DNA topoisomerase I, and DNA synthesis catalyzed by Taq DNA polymerase. Thus, the addition of the dangling amine groups resulting in structures of SI-PPCs, which differ so markedly from the derivatives of cisplatin used in the clinic, appears to contribute to the overall biological activity of these molecules.
Czech Academy of Sciences Institute of Biophysics Kralovopolska 135 CZ 61265 Brno Czech Republic
Department of Chemistry Virginia Commonwealth University Richmond Virginia 23284 2006 United States
References provided by Crossref.org
On the Biology of Werner's Complex
