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

Authors: Legigan, Thibaut; Clarhaut, Jonathan; Tranoy-Opalinski, Isabelle; Monvoisin, Arnaud; Renoux, Brigitte; Thomas, Mikael; Le Pape, Alain; Lerondel, Stephanie; Papot, Sebastien; Angewandte Chemie, International Edition; (2012); 10.1002/anie.201204935

Massive attack: Galactoside prodrugs have been designed that can be selectively activated by lysosomal ?-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.