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The First Generation of β‐Galactosidase‐Responsive Prodrugs Designed for the Selective Treatment of Solid Tumors in Prodrug Monotherapy

2012; Wiley; Volume: 51; Issue: 46 Linguagem: Inglês

10.1002/anie.201204935

1521-3773

Thibaut Legigan, Jonathan Clarhaut, Isabelle Tranoy‐Opalinski, Arnaud Monvoisin, Brigitte Renoux, Mikaël Thomas, Alain Le Pape, Stéphanie Lerondel, Sébastien Papot,

Cellular transport and secretion

Massive attack: Galactoside prodrugs have been designed that can be selectively activated by lysosomal β-galactosidase located inside cancer cells expressing a specific tumor-associated receptor. This efficient enzymatic process triggers a potent cytotoxic effect, releasing the potent antimitotic agent MMAE and allowing the destruction of both receptor-positive and surrounding receptor-negative tumor cells. Detailed facts of importance to specialist readers are published as "Supporting Information". Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.