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

ID: ALA4373672

Journal: Medchemcomm

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

Authors: Beekman AM, Cominetti MMD, Cartwright OC, Boger DL, Searcey M.

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.

CiteXplore: 32879717

DOI: 10.1039/C9MD00279K

Patent ID: ┄