Document Report Card

ID: ALA4368881

Journal: Medchemcomm

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

Authors: Renoux B, Fangous L, Hötten C, Péraudeau E, Eddhif B, Poinot P, Clarhaut J, Papot S.

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.

CiteXplore: 30746064

DOI: 10.1039/C8MD00466H