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

Brigitte Renoux Laure Fangous Camille Hötten Elodie Péraudeau Balkis Eddhif Pauline Poinot Jonathan Clarhaut Sébastien Papot

Medchemcomm

Institut de Chimie des Milieux et des Matériaux de Poitiers (IC2MP) , Université de Poitiers, CNRS, groupe "Systèmes Moléculaires Programmés" , 4 rue Michel Brunet, TSA 51106 , F-86073 Poitiers , France . Email:

Published: December 2018

We report on the synthesis, and 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.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6335994PMC
http://dx.doi.org/10.1039/c8md00466hDOI Listing

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