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  4. Metal-Based Inhibition of Poly(ADP-ribose) Polymerase - The Guardian Angel of DNA
 
research article

Metal-Based Inhibition of Poly(ADP-ribose) Polymerase - The Guardian Angel of DNA

Mendes, Filipa
•
Groessl, Michael  
•
Nazarov, Alexey A.  
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2011
Journal Of Medicinal Chemistry

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.

  • Details
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Type
research article
DOI
10.1021/jm2000135
Web of Science ID

WOS:000289215700019

Author(s)
Mendes, Filipa
Groessl, Michael  
Nazarov, Alexey A.  
Tsybin, Yury O.  
Sava, Gianni
Santos, Isabel
Dyson, Paul J.  
Casini, Angela  
Date Issued

2011

Publisher

American Chemical Society

Published in
Journal Of Medicinal Chemistry
Volume

54

Start page

2196

End page

2206

Subjects

Organometallic Ruthenium Compound

•

Platinum-Modified Dna

•

Mass-Spectrometry

•

Anticancer Drugs

•

Solution Chemistry

•

Nuclear Proteins

•

Zinc Fingers

•

Gold(Iii) Complexes

•

Binding Properties

•

Bipyridyl Ligands

Editorial or Peer reviewed

NON-REVIEWED

Written at

EPFL

EPFL units
LSMB  
LCOM  
Available on Infoscience
May 12, 2011
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/67305
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