A Reactive Antibody Platform for One-Step Production of Antibody-Drug Conjugates through a Diels-Alder Reaction with Maleimide

Bioconjug Chem. 2019 Sep 18;30(9):2340-2348. doi: 10.1021/acs.bioconjchem.9b00436. Epub 2019 Aug 19.

Abstract

The normal electron-demand Diels-Alder (DA) cycloaddition is a classic transformation routinely used in synthesis; however, applications in biological systems are limited. Here, we report a spiro[2.4]hepta-4,6-diene-containing noncanonical amino acid (SCpHK) capable of efficient incorporation into antibodies and subsequent coupling with maleimide via a DA reaction. SCpHK was stable throughout protein expression in mammalian cells and enabled covalent attachment of maleimide drug-linkers yielding DA antibody-drug conjugates (DA-ADCs) with nearly quantitative conversion in a one-step process. The uncatalyzed DA reaction between SCpHK and maleimide in aqueous buffer was rapid (1.8-5.4 M-1 s-1), and the antibody-drug adduct was stable in rat serum for at least 1 week at 37 °C. Anti-EphA2 DA-ADCs containing AZ1508 or SG3249 maleimide drug-linkers were potent inhibitors of tumor growth in PC3 tumor models in vivo. The DA bioconjugation strategy described here represents a simple method to produce site-specific and stable ADCs with maleimide drug-linkers.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cell Survival / drug effects
  • Cricetulus
  • Cycloaddition Reaction
  • Humans
  • Immunoconjugates / chemistry*
  • Immunoconjugates / pharmacology
  • Maleimides / chemistry*
  • Models, Molecular
  • PC-3 Cells
  • Protein Conformation
  • Spiro Compounds / chemistry

Substances

  • Immunoconjugates
  • Maleimides
  • Spiro Compounds
  • maleimide