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Issue 87, 2015
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A dendritic β-galactosidase-responsive folate–monomethylauristatin E conjugate

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Abstract

We report the study of a new drug delivery system programmed for the selective internalisation and the subsequent enzyme-catalysed release of two monomethylauristatin E molecules inside FR-positive cancer cells. This targeting device is the most potent β-galactosidase-responsive folate–drug conjugate developed so far, killing cancer cells expressing a medium level of FR at low nanomolar concentrations.

Graphical abstract: A dendritic β-galactosidase-responsive folate–monomethylauristatin E conjugate

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Supplementary files

Article information


Submitted
27 Jun 2015
Accepted
08 Sep 2015
First published
08 Sep 2015

Chem. Commun., 2015,51, 15792-15795
Article type
Communication
Author version available

A dendritic β-galactosidase-responsive folate–monomethylauristatin E conjugate

J. Alsarraf, E. Péraudeau, P. Poinot, I. Tranoy-Opalinski, J. Clarhaut, B. Renoux and S. Papot, Chem. Commun., 2015, 51, 15792
DOI: 10.1039/C5CC05294G

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