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Metal-based inhibition of poly(ADP-ribose) polymerase: the guardian angel of DNA

Mendes, Filipa, Groessl, Michael, Nazarov, Alexey A., Tsybin, Yury O., Sava, Gianni, Santos, Isabel, Dyson, Paul J. and Casini, Angela 2011. Metal-based inhibition of poly(ADP-ribose) polymerase: the guardian angel of DNA. Journal of Medicinal Chemistry 54 (7) , pp. 2196-2206. 10.1021/jm2000135

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The inhibition activity of a series of anticancer metal complexes based on platinum, ruthenium, and gold metal ions was evaluated on the zinc-finger protein PARP-1, either purified or directly on protein extracts from human breast cancer MCF7 cells. Information on the reactivity of the metal complexes with the PARP-1 zinc-finger domain was obtained by high-resolution ESI FT-ICR mass spectrometry. An excellent correlation between PARP-1 inhibition in protein extracts and the ability of the complexes to bind to the zinc-finger motif (in competition with zinc) was established. The results support a model whereby displacement of zinc from the PARP-1 zinc finger by other metal ions leads to decreased PARP-1 activity. In vitro combination studies of cisplatin with NAMI-A and RAPTA-T on different cancer cell lines (MCF7, A2780, and A2780cisR) showed that, in some cases, a synergistic effect is in operation.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Publisher: American Chemical Society
Last Modified: 23 Jul 2020 01:44

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