Synthesis of a Self-Adjuvanting MUC1 Vaccine via Diselenide-Selenoester Ligation-Deselenization

ACS Chem Biol. 2018 Dec 21;13(12):3279-3285. doi: 10.1021/acschembio.8b00675. Epub 2018 Nov 14.

Abstract

Access to lipopeptide-based vaccines for immunological studies remains a significant challenge owing to the amphipathic nature of the molecules, which makes them difficult to synthesize and purify to homogeneity. Here, we describe the application of a new peptide ligation technology, the diselenide-selenoester ligation (DSL), to access self-adjuvanting glycolipopeptide vaccines. We show that rapid ligation of glyco- and lipopeptides is possible via DSL in mixed organic solvent-aqueous buffer and, when coupled with deselenization chemistry, affords rapid and efficient access to a vaccine candidate possessing a MUC1 glycopeptide epitope and the lipopeptide adjuvant Pam2Cys. This construct was shown to elicit MUC1-specific antibody and cytotoxic T lymphocyte responses in the absence of any other injected lipids or adjuvants. The inclusion of the helper T cell epitope PADRE both boosted the antibody response and resulted in elevated cytokine production.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adjuvants, Immunologic / chemical synthesis*
  • Amino Acid Sequence
  • Animals
  • Cancer Vaccines / chemical synthesis
  • Cancer Vaccines / immunology*
  • Chemistry Techniques, Synthetic / methods
  • Female
  • Glycopeptides / chemical synthesis
  • Glycopeptides / immunology*
  • Humans
  • Lipopeptides / chemical synthesis
  • Lipopeptides / immunology*
  • MCF-7 Cells
  • Mice, Inbred C57BL
  • Minisatellite Repeats
  • Mucin-1 / genetics
  • Mucin-1 / immunology*
  • Organoselenium Compounds / chemical synthesis
  • Organoselenium Compounds / chemistry*

Substances

  • Adjuvants, Immunologic
  • Cancer Vaccines
  • Glycopeptides
  • Lipopeptides
  • MUC1 protein, human
  • Mucin-1
  • Organoselenium Compounds