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

Autor: Romain Barat, Isabelle Tranoy-Opalinski, Antony E. Fernandes, Vincent Aucagne, Sébastien Papot, Jonathan Clarhaut, Thibaut Legigan, Pauline Poinot, Elodie Péraudeau, Brigitte Renoux, David A. Leigh
Přispěvatelé: Institut de Chimie des Milieux et Matériaux de Poitiers (IC2MP), Université de Poitiers-Centre National de la Recherche Scientifique (CNRS), Signalisation et Transports Ioniques Membranaires (STIM), Université de Tours-Université de Poitiers-Centre National de la Recherche Scientifique (CNRS), Centre hospitalier universitaire de Poitiers (CHU Poitiers), Institut de la matière condensée et des nanosciences / Institute of Condensed Matter and Nanosciences (IMCN), Université Catholique de Louvain (UCL), Centre de biophysique moléculaire (CBM), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), School of Chemistry, University of Manchester [Manchester], UCL - SST/IMCN/BSMA - Bio and soft matter, Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université de Poitiers-Institut de Chimie du CNRS (INC), Université de Poitiers-Université de Tours (UT)-Centre National de la Recherche Scientifique (CNRS), Université Catholique de Louvain = Catholic University of Louvain (UCL), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Université de Poitiers-Université de Tours-Centre National de la Recherche Scientifique (CNRS), Université de Poitiers-Institut national des sciences de l'Univers (INSU - CNRS)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), TRANOY, isabelle
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Zdroj: Chemical Science
Chemical Science, The Royal Society of Chemistry, 2015, 6 (4), pp.2608-2613. ⟨10.1039/C5SC00648A⟩
Chemical Science : a new journal for findings of exceptional significance from across the chemical sciences, Vol. 6, no.4, p. 2608-2613 (2015)
Chemical Science, The Royal Society of Chemistry, 2015, 6 (4), pp.2608-2613. ⟨10.1039/c5sc00648a⟩
Chemical Science, 2015, 6 (4), pp.2608-2613. ⟨10.1039/c5sc00648a⟩
ISSN: 2041-6520
2041-6539
Popis: International audience; 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.
Databáze: OpenAIRE
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