Structure of the 4-1BB/4-1BBL complex and distinct binding and functional properties of utomilumab and urelumab

Nat Commun. 2018 Nov 8;9(1):4679. doi: 10.1038/s41467-018-07136-7.

Abstract

4-1BB (CD137, TNFRSF9) is an inducible costimulatory receptor expressed on activated T cells. Clinical trials of two agonist antibodies, utomilumab (PF-05082566) and urelumab (BMS-663513), are ongoing in multiple cancer indications, and both antibodies demonstrate distinct activities in the clinic. To understand these differences, we solved structures of the human 4-1BB/4-1BBL complex, the 4-1BBL trimer alone, and 4-1BB bound to utomilumab or urelumab. The 4-1BB/4-1BBL complex displays a unique interaction between receptor and ligand when compared with other TNF family members. Furthermore, our ligand-only structure differs from previously published data. Utomilumab, a ligand-blocking antibody, binds 4-1BB between CRDs 3 and 4. In contrast, urelumab binds 4-1BB CRD-1, away from the ligand binding site. Finally, cell-based assays demonstrate utomilumab is a milder agonist than urelumab. Collectively, our data provide a deeper understanding of the 4-1BB signaling complex, providing a template for future development of next generation 4-1BB targeted biologics.

Publication types

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

MeSH terms

  • 4-1BB Ligand / chemistry*
  • 4-1BB Ligand / metabolism*
  • Antibodies, Monoclonal / chemistry*
  • Antibodies, Monoclonal / metabolism*
  • Antibodies, Monoclonal, Humanized
  • Binding Sites
  • HEK293 Cells
  • Humans
  • Immunoglobulin G / chemistry*
  • Immunoglobulin G / metabolism*
  • Jurkat Cells
  • Models, Molecular
  • Protein Domains
  • Tumor Necrosis Factor Receptor Superfamily, Member 9 / chemistry*
  • Tumor Necrosis Factor Receptor Superfamily, Member 9 / metabolism*

Substances

  • 4-1BB Ligand
  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Immunoglobulin G
  • Tumor Necrosis Factor Receptor Superfamily, Member 9
  • urelumab
  • utomilumab