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Eur J Med Chem. 2013 Sep;67:75-80. doi: 10.1016/j.ejmech.2013.06.037. Epub 2013 Jun 25.

Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy.

Author information

  • 1Université de Poitiers, UMR-CNRS 7285, Institut de Chimie des Milieux et des Matériaux de Poitiers (IC2MP), Groupe "Systèmes Moléculaires Programmés", 4 rue Michel Brunet, 86022 Poitiers, France.

Abstract

We developed a glucuronide prodrug of the potent monomethylauristatin E (MMAE). This prodrug is significantly less toxic than the parent drug. However, in the presence of β-glucuronidase the prodrug leads to the efficient release of MMAE thereby triggering a subnanomolar cytotoxic activity against several cancer cell lines. Preliminary in vivo experiments conducted in C57BL/6 mice bearing a subcutaneous murine Lewis Lung Carcinoma (LLC) demonstrated the potential of this targeting system for the selective treatment of solid tumors.

Copyright © 2013 Elsevier Masson SAS. All rights reserved.

KEYWORDS:

Cancer; Chemotherapy; Glucuronide; Prodrug; Tumor targeting

PMID:
23845743
[PubMed - indexed for MEDLINE]
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