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Updated: Dec 10, 2025

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
A small molecule drug conjugate (SMDC) of DUPA and a duocarmycin built on the solid phase
Andrew Michael Beekman1, Marco M D Cominetti1, Oliver Charles Cartwright1
1School of Pharmacy & School of Chemistry , University of East Anglia , Norwich Research Park, Norwich , Norfolk , NR47TJ , UK . Email: A.Beekman@uea.ac.uk ;
Abstract:
In a proof-of-concept study, solid phase synthesis allowed the rapid generation of a small molecule drug conjugate in which the glutamate carboxypeptidase II (GCPII) targeting small molecule DUPA was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The targeted SMDC contained a cathepsin B cleavable linker, which was shown to be active and selective against cathepsin B over-expressing and GCPII-expressing tumour cell lines.
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