Journal
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
Volume 15, Issue 6, Pages 841-850Publisher
SPRINGER
DOI: 10.1007/s00775-010-0648-8
Keywords
Platinum complexes; Phosphanes and amines; DNA quadruplex; Telomere; Cytotoxicity
Funding
- Regione Piemonte [A 370]
- ATF Association (Alessandria, Italy)
- CNRS
- ARC, (Paris, France) [4835]
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Enantiomeric complexes of formula [PtCl2L2] [L-2 is (R)-(+)-BINAP and (S)-(-)-BINAP, where BINAP is 2,2'-bis(diphenylphosphane)-1,1'-binaphthyl, and (R)-(+)-DABN and (S)-(-)-DABN, where DABN is 1,1'-binaphthyl-2,2'-diamine], were tested for their cytotoxic activity against three cancer cell lines and for their ability to bind to the human telomeric sequence folded in the G-quadruplex structure. Similar experiments were carried out on prototypal complexes cisplatin and cis-[PtCl2(PPh3)(2)] for comparison. Platinum complexes containing phosphanes proved less cytotoxic to cancer cell lines and less likely to interact with the nucleobases of the G-quadruplex than those containing amines; in both cases the S-(-) isomer was more active than the R-(+) counterpart. More specifically, whereas all the platinum complexes were able to platinate the G-quadruplex structure from the human telomeric repeat, the extent and sites of platination depended on the nature of the ligands. Complexes containing (bulky) phosphanes interacted only with the adenines of the loops, whereas those containing the less sterically demanding amines interacted with adenines and some guanines of the G-quartet.
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