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A dendritic β-galactosidase-responsive folate-monomethylauristatin E conjugate
Jérôme Alsarraf1, Elodie Péraudeau2, Pauline Poinot3
1Université de Poitiers, UMR-CNRS 7285, Institut de Chimie des Milieux et des Matériaux de Poitiers, groupe "Systèmes Moléculaires Programmés", 4 rue Michel Brunet, TSA 51106, 86073 Poitiers, France. sebastien.papot@univ-poitiers.fr.
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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