A new paclitaxel prodrug for use in ADEPT strategy |
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Authors: | Bouvier Emmanuel Thirot Sylvie Schmidt Frédéric Monneret Claude |
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Institution: | UMR 176 CNRS-Institut Curie, Section Recherche 26 rue d'Ulm, 75248 Paris Cedex 05, France. |
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Abstract: | A new paclitaxel prodrug intended for use in Antibody-Directed Prodrug Therapy (ADEPT) or Prodrug Monotherapy (PMT) has been prepared. This prodrug was originally designed to be activated into the drug by human beta-glucuronidase. In order to enhance the liberation rate of paclitaxel, an elongated spacer system including a nitro-aromatic derivative and a N,N'-methylethylenediamine was incorporated between the sugar moiety and the drug. Indeed, this new prodrug proved to be activated significantly faster than a former paclitaxel prodrug containing a conventional spacer. |
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