A small molecule drug conjugate (SMDC) of DUPA and a duocarmycin built on the solid phase

Andrew Beekman, Marco Cominetti, Oliver Cartwright, Dale L. Boger, Mark Searcey

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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.
Original languageEnglish
Pages (from-to)2170-2174
Number of pages5
JournalMedChemComm
Volume10
Issue number12
Early online date27 Nov 2019
DOIs
Publication statusPublished - Dec 2019

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