Issue 4, 2015

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 β-galactosidase.

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

Supplementary files

Article information

Article type
Edge Article
Submitted
20 ก.พ. 2558
Accepted
23 ก.พ. 2558
First published
25 ก.พ. 2558
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2015,6, 2608-2613

Author version available

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

R. Barat, T. Legigan, I. Tranoy-Opalinski, B. Renoux, E. Péraudeau, J. Clarhaut, P. Poinot, A. E. Fernandes, V. Aucagne, D. A. Leigh and S. Papot, Chem. Sci., 2015, 6, 2608 DOI: 10.1039/C5SC00648A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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