Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)

Chem Commun (Camb). 2015 Jul 7;51(53):10624-7. doi: 10.1039/c5cc03557k. Epub 2015 Jun 5.

Abstract

Herein we report the use of next generation maleimides (NGMs) for the construction of a potent antibody-drug conjugate (ADC) via functional disulfide bridging. The linker has excellent stability in blood serum and the ADC, armed with monomethyl auristatin E (MMAE), shows excellent potency and cancer cell selectivity in vitro.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Monoclonal / chemistry*
  • Cell Proliferation / drug effects
  • Click Chemistry
  • Disulfides / chemistry*
  • Fluorescent Dyes / chemistry
  • Humans
  • Immunoconjugates / chemistry*
  • Immunoconjugates / toxicity
  • MCF-7 Cells
  • Oligopeptides / chemistry*
  • Trastuzumab / chemistry

Substances

  • Antibodies, Monoclonal
  • Disulfides
  • Fluorescent Dyes
  • Immunoconjugates
  • Oligopeptides
  • Trastuzumab
  • monomethyl auristatin E