Journal
CHEMICAL SCIENCE
Volume 6, Issue 4, Pages 2608-2613Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5sc00648a
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Funding
- CNRS
- Region Poitou-Charentes
- La Ligue contre le Cancer (Comites Vienne and Deux-Sevres)
- Sport et Collection
- Agence Nationale de la Recherche (ANR) [Blanc-SIMI 7]
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The development of mechanically interlocked molecular systems programmed to operate autonomously in biological environments is an emerging field of research with potential medicinal applications. Within this framework, functional rotaxane- and pseudorotaxane-based architectures are starting to attract interest for the delivery of anticancer drugs, with the ultimate goal to improve the efficiency of cancer chemotherapy. Here, we report an enzyme-sensitive [2]-rotaxane designed to release a potent anticancer drug within tumor cells. The molecular device includes a protective ring that prevents the premature liberation of the drug in plasma. However, once located inside cancer cells the [2]-rotaxane leads to the release of the drug through the controlled disassembly of the mechanically interlocked components, in response to a determined sequence of two distinct enzymatic activations. Furthermore, in vitro biological evaluations reveal that this biocompatible functional system exhibits a noticeable level of selectivity for cancer cells overexpressing beta-galactosidase.
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