albumin - publications

1. J Med Chem. 2012 Apr 19. [Epub ahead of print]

Synthesis and Antitumor Efficacy of a -Glucuronidase-Responsive Albumin-Binding
Prodrug of Doxorubicin.

Legigan T, Clarhaut J, Renoux B, Tranoy-Opalinski I, Monvoisin A, Berjeaud JM,
Guilhot F, Papot S.

In this paper we describe the synthesis and biological evaluation of the first
-glucuronidase-responsive albumin-binding prodrug designed for the selective
delivery of doxorubicin at the tumor site. This prodrug leads to superior
antitumor efficacy in mice compared to HMR 1826, a well-known glucuronide prodrug
of doxorubicin which can not bind covalently to circulating albumin. Furthermore,
this compound inhibits tumor growth in a similar manner to doxorubicin whilst
avoiding side effects induced by the free drug.

PMID: 22515366 [PubMed - as supplied by publisher]