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A β-glucuronidase-responsive albumin-binding prodrug programmed for the double release of monomethyl auristatin E

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Abstract

We report on the synthesis, in vitro and in vivo biological evaluations of a dimeric β-glucuronidase-responsive albumin-binding prodrug designed for the double release of MMAE upon a single enzymatic activation step. This prodrug produced a significant antitumour activity in mice bearing subcutaneous LS174T colorectal adenocarcinoma xenografts without inducing side effects.

Graphical abstract: A β-glucuronidase-responsive albumin-binding prodrug programmed for the double release of monomethyl auristatin E

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Publication details

The article was received on 14 Sep 2018, accepted on 25 Oct 2018 and first published on 26 Oct 2018


Article type: Research Article
DOI: 10.1039/C8MD00466H
Citation: Med. Chem. Commun., 2018, Advance Article
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    A β-glucuronidase-responsive albumin-binding prodrug programmed for the double release of monomethyl auristatin E

    B. Renoux, L. Fangous, C. Hötten, E. Péraudeau, B. Eddhif, P. Poinot, J. Clarhaut and S. Papot, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00466H

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