Antibody-mimetic ligand selected by mRNA display targets DC-SIGN for dendritic cell-directed antigen delivery

ACS Chem Biol. 2013 May 17;8(5):967-77. doi: 10.1021/cb300680c. Epub 2013 Mar 8.

Abstract

Dendritic cell (DC)-based vaccines have shown promise as an immunotherapeutic modality for cancer and infectious diseases in many preclinical studies and clinical trials. Provenge (sipuleucel-T), a DC-based vaccine based on ex vivo-generated autologous DCs loaded with antigens, has recently received FDA approval for prostate cancer treatment, further validating the potential of DC-based vaccine modalities. However, direct antigen delivery to DCs in vivo via DC-specific surface receptors would enable a more direct and less laborious approach to immunization. In this study, the recombinant extracellular domains (ECD) of human and mouse DC-SIGN (hDC-SIGN and mDC-SIGN) were generated as DC-specific targets for mRNA display. Accordingly, an antibody-mimetic library was constructed by randomizing two exposed binding loops of an expression-enhanced 10th human fibronectin type III domain (e10Fn3). After three rounds of selection against mDC-SIGN, followed by four rounds of selection against hDC-SIGN, we were able to evolve several dual-specific ligands, which could bind to both soluble ECD of human and mouse DC-SIGNs. Using a cell-binding assay, one ligand, eFn-DC6, was found to have high affinity to hDC-SIGN and moderate affinity to mDC-SIGN. When fused with an antigenic peptide, eFn-DC6 could direct the antigen delivery and presentation by human peripheral blood mononuclear cell (PBMC)-derived DCs and stimulate antigen-specific CD8(+) T cells to secrete inflammatory cytokines. Taken together, these results demonstrate the utility of mRNA display to select protein carriers for DC-based vaccination and offer in vitro evidence that the antibody-mimetic ligand eFn-DC6 represents a promising candidate for the development of an in vivo DC-based vaccine in humans.

Publication types

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

MeSH terms

  • Animals
  • Antibodies / immunology
  • Antigens / administration & dosage*
  • Antigens / genetics
  • Base Sequence
  • Binding Sites
  • Biomimetic Materials
  • Cell Adhesion Molecules / genetics*
  • Cell Adhesion Molecules / metabolism
  • Cell Surface Display Techniques / methods*
  • Dendritic Cells / immunology*
  • Dendritic Cells / metabolism
  • Drug Delivery Systems / methods*
  • Fibronectins / genetics
  • Fibronectins / metabolism
  • Humans
  • Lectins, C-Type / genetics*
  • Lectins, C-Type / metabolism
  • Ligands
  • Mice
  • Molecular Sequence Data
  • RNA, Messenger / immunology
  • RNA, Messenger / metabolism*
  • Receptors, Cell Surface / genetics*
  • Receptors, Cell Surface / metabolism
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism

Substances

  • Antibodies
  • Antigens
  • Cell Adhesion Molecules
  • DC-specific ICAM-3 grabbing nonintegrin
  • Fibronectins
  • Lectins, C-Type
  • Ligands
  • RNA, Messenger
  • Receptors, Cell Surface
  • Recombinant Proteins
  • fibronectin type III like peptide, human