A mechanically interlocked molecular system programmed for the delivery of an anticancer drug

Abstract : 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 [small beta]-galactosidase.
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Journal articles
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https://hal.archives-ouvertes.fr/hal-01170448
Contributor : Isabelle Frapart <>
Submitted on : Wednesday, July 1, 2015 - 3:36:50 PM
Last modification on : Tuesday, April 2, 2019 - 5:28:03 PM

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Romain Barat, Thibaut Legigan, Isabelle Tranoy-Opalinski, Brigitte Renoux, Elodie Péraudeau, et al.. A mechanically interlocked molecular system programmed for the delivery of an anticancer drug. Chemical Science , The Royal Society of Chemistry, 2015, 6 (4), pp.2608-2613. ⟨10.1039/C5SC00648A⟩. ⟨hal-01170448⟩

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