Crystal structure of the human LAG-3-HLA-DR1-peptide complex

Sci Immunol. 2024 Dec 13;9(102):eads5122. doi: 10.1126/sciimmunol.ads5122. Epub 2024 Dec 13.

Abstract

T cell activity is governed by T cell receptor (TCR) signaling and constrained by immune checkpoint molecules, including programmed cell death protein 1 (PD-1), cytotoxic T lymphocyte-associated antigen 4 (CTLA-4), and lymphocyte activation gene 3 (LAG-3). The basis for how LAG-3 binds to human leukocyte antigen class II molecules (HLA-II) remains unknown. Here, we present the 3.4-angstrom crystal structure of a LAG-3-peptide-HLA-II complex and probe the energetics of the complex interface. Coincident with the HLA-II binding site of the ancestrally related, monomeric CD4 receptor, the LAG-3 homodimer laterally engages two HLA-II molecules via distal D1 domain surfaces, imposing a 38° angular offset. The LAG-3-HLA-II interface is discontinuous and lacks involvement of the D1 extra loop, a binding site for anti-LAG-3 therapeutic monoclonal antibodies. Upon HLA-II binding, intrinsically mobile loops of the LAG-3 molecule become ordered, with contact residues highly conserved across HLA-DR, DQ, and DP allomorphs. Our data provide a structural foundation for development of immunomodulatory approaches targeting LAG-3.

MeSH terms

  • Antigens, CD* / chemistry
  • Antigens, CD* / immunology
  • Antigens, CD* / metabolism
  • Crystallography, X-Ray
  • HLA-DR1 Antigen* / chemistry
  • HLA-DR1 Antigen* / immunology
  • Humans
  • Lymphocyte Activation Gene 3 Protein*
  • Models, Molecular
  • Peptides / chemistry
  • Peptides / immunology
  • Protein Binding

Substances

  • Lymphocyte Activation Gene 3 Protein
  • Antigens, CD
  • Lag3 protein, human
  • HLA-DR1 Antigen
  • Peptides