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Inside Cover: The First Generation of β‐Galactosidase‐Responsive Prodrugs Designed for the Selective Treatment of Solid Tumors in Prodrug Monotherapy (Angew. Chem. Int. Ed. 46/2012)
Author(s) -
Legigan Thibaut,
Clarhaut Jonathan,
TranoyOpalinski Isabelle,
Monvoisin Arnaud,
Renoux Brigitte,
Thomas Mikaël,
Le Pape Alain,
Lerondel Stéphanie,
Papot Sébastien
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201207805
Subject(s) - prodrug , int , chemistry , cytotoxic t cell , receptor , cancer research , enzyme , pharmacology , combinatorial chemistry , biochemistry , biology , in vitro , computer science , operating system
A galactoside prodrug has been designed that can be selectively activated by lysosomal β‐galactosidase located inside cancer cells expressing a specific tumor‐associated receptor. In their Communication on page 11606 ff . S. Papot and co‐workers show that 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.