title: Study of a cyclopamine glucuronide prodrug for the selective chemotherapy of glioblastoma.
abstract: The first glucuronide prodrug of the hedgehog signaling inhibitor cyclopamine was synthesized. The carbamoyl derivatisation of cyclopamine significantly decreased its toxicity towards the U87 human glioblastoma cell line. However, when the prodrug was incubated with beta-glucuronidase in the culture media, the active drug was efficiently released thereby restoring its anti-proliferative activity.
authors.affiliation: Université de Poitiers, UMR-CNRS 6514, 40 avenue du Recteur Pineau, 86022 Poitiers, France.
authors.forename: Florian
authors.initials: F
authors.lastname: Hamon
authors.forename: Brigitte
authors.initials: B
authors.lastname: Renoux
authors.forename: Corinne
authors.initials: C
authors.lastname: Chadéneau
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Muller
authors.forename: Sébastien
authors.initials: S
authors.lastname: Papot
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D005909:Glioblastoma / Q000188:drug therapy* / Q000473:pathology; D020719:Glucuronides / Q000737:chemistry*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011355:Prodrugs / Q000627:therapeutic use*; D021241:Spectrometry, Mass, Electrospray Ionization; D014704:Veratrum Alkaloids / Q000737:chemistry / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D020719:Glucuronides; D011355:Prodrugs; D014704:Veratrum Alkaloids; C000541:cyclopamine