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

Beekman, Andrew ORCID: https://orcid.org/0000-0002-3056-6406, Cominetti, Marco, Cartwright, Oliver, Boger, Dale L. and Searcey, Mark ORCID: https://orcid.org/0000-0003-2273-8949 (2019) A small molecule drug conjugate (SMDC) of DUPA and a duocarmycin built on the solid phase. MedChemComm, 10 (12). pp. 2170-2174. ISSN 2040-2503

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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.

Item Type:	Article
Faculty \ School:	Faculty of Science > School of Pharmacy (former - to 2024)
UEA Research Groups:	Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021)
Depositing User:	LivePure Connector
Date Deposited:	13 Dec 2019 03:18
Last Modified:	25 Sep 2024 14:23
URI:	https://ueaeprints.uea.ac.uk/id/eprint/73364
DOI:	10.1039/C9MD00279K

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