Determination of the mechanism of action of anti-FasL antibody by epitope mapping and homology modeling

Biochemistry. 2009 Aug 4;48(30):7251-60. doi: 10.1021/bi900296g.

Abstract

Fas ligand (FasL) is a 40-kDa type II transmembrane protein belonging to the tumor necrosis factor (TNF) family of proteins and binds to its specific receptor, Fas, a member of the TNF receptor family. Membrane-bound FasL can be processed into a soluble form by a metalloprotease similar to that which cleaves TNFalpha. Elevated levels of FasL have been implicated in a wide variety of diseases ranging from cancer to inflammatory abnormalities, which could be targeted by antibody therapy. We generated a fully human high-affinity antibody against FasL that binds to and neutralizes the activity of both soluble and membrane-associated human FasL. In order to elucidate the mechanism of function of this antibody, we have mapped the region and critical residues involved in the recognition of FasL using a combination of homology modeling, immunoprecipitation, hydrogen-deuterium exchange mass spectrometry (H/DXMS), and alanine scanning site-directed mutagenesis. These studies have revealed the antibody binding site on human FasL. Furthermore, through molecular homology modeling, we have proposed a mechanism for the neutralizing activity of this antibody that involves interference with the docking of the ligand to its receptor by the antibody.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies* / chemistry
  • Antibodies* / immunology
  • Apoptosis / immunology
  • Binding Sites
  • Epitope Mapping
  • Epitopes / chemistry*
  • Epitopes / immunology
  • Fas Ligand Protein / chemistry*
  • Fas Ligand Protein / genetics
  • Fas Ligand Protein / immunology*
  • Humans
  • Jurkat Cells
  • Mice
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Protein Binding
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / immunology
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
  • Trypsin / metabolism

Substances

  • Antibodies
  • Epitopes
  • Fas Ligand Protein
  • Recombinant Fusion Proteins
  • Trypsin