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

Bioconjug Chem. 2020 Jul 15;31(7):1745-1749. doi: 10.1021/acs.bioconjchem.0c00282. Epub 2020 Jun 15.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antigens, Tumor-Associated, Carbohydrate / drug effects*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Duocarmycins / chemistry*
  • Humans
  • Peptides / chemistry*

Substances

  • Antigens, Tumor-Associated, Carbohydrate
  • Antineoplastic Agents
  • Duocarmycins
  • Peptides
  • Thomsen-Friedenreich antigen