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

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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.

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

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Publication details

The article was received on 15 May 2019, accepted on 12 Nov 2019 and first published on 27 Nov 2019


Article type: Research Article
DOI: 10.1039/C9MD00279K
Med. Chem. Commun., 2019, Advance Article

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

    A. M. Beekman, M. M. D. Cominetti, O. C. Cartwright, D. L. Boger and M. Searcey, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9MD00279K

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