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.

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Alsarraf, J., Péraudeau, E., Poinot, P., Tranoy-Opalinski, I., Clarhaut, J., Renoux, B., & Papot, S. (2015). A dendritic β-galactosidase-responsive folate-monomethylauristatin e conjugate. Chemical Communications, 51(87), 15792–15795. https://doi.org/10.1039/c5cc05294g

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