title: The first generation of β-galactosidase-responsive prodrugs designed for the selective treatment of solid tumors in prodrug monotherapy.
abstract: 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.
authors.affiliation: Université de Poitiers, UMR-CNRS 7285, Institut de Chimie des Milieux et des Matériaux de Poitiers, Groupe Systèmes Moléculaires Programmés, 4 rue Michel Brunet, 86022 Poitiers, France.
authors.forename: Thibaut
authors.initials: T
authors.lastname: Legigan
authors.forename: Jonathan
authors.initials: J
authors.lastname: Clarhaut
authors.forename: Isabelle
authors.initials: I
authors.lastname: Tranoy-Opalinski
authors.forename: Arnaud
authors.initials: A
authors.lastname: Monvoisin
authors.forename: Brigitte
authors.initials: B
authors.lastname: Renoux
authors.forename: Mikaël
authors.initials: M
authors.lastname: Thomas
authors.forename: Alain
authors.initials: A
authors.lastname: Le Pape
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Lerondel
authors.forename: Sébastien
authors.initials: S
authors.lastname: Papot
mesh_terms: D062365:Aminobenzoates / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000473:pathology; D009842:Oligopeptides / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D011355:Prodrugs / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*; D001616:beta-Galactosidase / Q000378:metabolism*
chemical_list: D062365:Aminobenzoates; D000970:Antineoplastic Agents; D009842:Oligopeptides; D011355:Prodrugs; C543533:auristatin; D001616:beta-Galactosidase