Elimination of a human T-cell region in staphylokinase by T-cell screening and computer modeling

Thromb Haemost. 2002 Apr;87(4):666-73.

Abstract

Staphylokinase is a potent highly fibrin-selective thrombolytic agent, but it induces a humoral immune response in most treated patients. Staphylokinase-specific T-lymphocytes can be found in normal healthy individuals, from whom a large panel of staphylokinase-specific T-cells were cloned. The staphylokinase amino acid sequence 71-87 was widely recognized, as it induced proliferation of T-cell clones isolated from 90% of the donors. Computer modeling of this area, threaded as 11-mer peptides within the peptide-binding groove of the major HLA-DR alleles, indicated two putative partially overlapping binding sequences. The region-(71-87)-specific T-cell clones recognized either one or the other minimal peptide, confirming that both sequences could be functional T-cell epitopes. Furthermore, to guide the mutagenesis to eliminate T-cell reactivity, the contribution of each residue to the HLA-DR-anchoring and T-cell receptor exposure was evaluated for both binding motifs. Computer calculations combined with functional assays resulted in the design of staphylokinase-variants, including 2 to 4 amino acid substitutions in the region 71-87. These variants were no longer recognized by the region-(71-87)-specific T-cell clones, and importantly no new staphylokinase-variant-specific cellular immune response could be measured.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antigens, Bacterial / chemistry
  • Antigens, Bacterial / genetics
  • Antigens, Bacterial / immunology*
  • Binding Sites
  • Computer Simulation*
  • Drug Design
  • Epitopes / chemistry
  • Epitopes / immunology
  • Fibrinolytic Agents / chemistry
  • Fibrinolytic Agents / immunology*
  • HLA-DR Antigens / immunology
  • Humans
  • Lymphocyte Activation
  • Metalloendopeptidases / chemistry
  • Metalloendopeptidases / genetics
  • Metalloendopeptidases / immunology*
  • Models, Molecular*
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Oligopeptides / chemistry
  • Oligopeptides / immunology
  • Protein Conformation
  • T-Lymphocyte Subsets / immunology*

Substances

  • Antigens, Bacterial
  • Epitopes
  • Fibrinolytic Agents
  • HLA-DR Antigens
  • Oligopeptides
  • Metalloendopeptidases
  • auR protein, Staphylococcus aureus