Structural investigation of cyclo-dioxo maleimide cross-linkers for acid and serum stability

Org Biomol Chem. 2017 Nov 15;15(44):9305-9310. doi: 10.1039/c7ob01757j.

Abstract

The biochemical characteristics of hetero-bifunctional cross-linkers used in bioconjugates are of essential importance to the desired features of the final adduct (i.e. antibody-drug conjugates). These include stability in biological media, chemical and biological reactivities, cleavability under defined conditions, and solubility. In our previous work, we introduced a new amino-to-thiol linker, maleimidomethyl dioxane (MD), as an alternative to classical maleimide conjugation, with increased hydrophilicity and serum stability due to succinimidyl ring-opening. In this work, we investigate the generality of linkers containing a dioxo-ring with regard to their ability to self-hydrolyze and their surprising stability at a low pH. We synthesized four FRET probes which allowed us to address the stability of the dioxo-ring and to study the maleimide ring-opening and the thiol-exchange processes by means of detecting and measuring the generation of fluorescence. It was found that the ring expansion (from a 5- to a 6-membered ring) improved the stability of the probes in aqueous media, and the increase of the chain length between the dioxo-ring and the succinimide ring (from methylene to ethylene) decreased the rate of succinimidyl ring-opening.

MeSH terms

  • Drug Stability
  • Humans
  • Hydrogen-Ion Concentration
  • Maleimides / blood
  • Maleimides / chemistry*
  • Models, Molecular
  • Protein Conformation
  • Pyrans / chemistry
  • Serum Albumin, Human / chemistry
  • Sulfhydryl Compounds / chemistry
  • Water / chemistry

Substances

  • Maleimides
  • Pyrans
  • Sulfhydryl Compounds
  • Water
  • maleimide
  • Serum Albumin, Human