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First-in-Class Combination Therapy of a Copper(II) Metallo-Phosphorus Dendrimer with Cytotoxic Agents

Authors
  • Mignani, Serge
  • El Brahmi, Nabil
  • Cresteil, Thierry
  • Majoral, Jean-Pierre
Type
Published Article
Journal
Oncology
Publisher
S. Karger AG
Publication Date
Mar 13, 2018
Volume
94
Issue
5
Pages
324–328
Identifiers
DOI: 10.1159/000486680
PMID: 29533961
Source
Karger
Keywords
License
Green
External links

Abstract

The metallo-phosphorus dendrimer 1G3-Cu (generation 3 dendrimer bearing 48 conjugated copper(II) on its surface) has antiproliferative activity related to its capacity to activate Bax translocation. In the present study, we evaluate the activity of an association of 1G3-Cu with 5 cytotoxic agents used in chemotherapy having different modes of action. Data show no additive effect with camptothecin and cisplatin, additivity with paclitaxel and MG132, and synergy with doxorubicin. Results suggest that the multivalent Cu-conjugated dendrimer 1G3-Cu (activator of Bax translocation) plays an important role in boosting the clinical impact of Bax accumulation stimulated by the proteasome inhibitor MG132, antimitotic taxanes, and the topo II inhibitor doxorubicin.

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