A Peptide-Duocarmycin Conjugate Targeting the Thomsen-Friedenreich Antigen Has Potent and Selective Antitumor Activity.

Bioconjugate Chemistry
Oliver Charles CartwrightMark Searcey

Abstract

Solid-phase synthesis allowed the rapid generation of a peptide-drug conjugate. A peptide targeting the Thomsen-Friedenreich antigen (TFα) was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The compound, containing a cathepsin B cleavable linker, was shown to be active and selective against TFα expressing tumor cell lines.

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Citations

Nov 25, 2020·Drug Discovery Today·Zoë JukesKlaus Pors
Jan 9, 2021·Journal of Medicinal Chemistry·Chunlei WuLijing Fang

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