Epitope characterization and crystal structure of GA101 provide insights into the molecular basis for type I/II distinction of CD20 antibodies

Blood. 2011 Jul 14;118(2):358-67. doi: 10.1182/blood-2010-09-305847. Epub 2011 Mar 28.

Abstract

CD20 is a cell-surface marker of normal and malignant B cells. Rituximab, a monoclonal antibody targeting CD20, has improved the treatment of malignant lymphomas. Therapeutic CD20 antibodies are classified as either type I or II based on different mechanisms of killing malignant B cells. To reveal the molecular basis of this distinction, we fine-mapped the epitopes recognized by both types. We also determined the first X-ray structure of a type II antibody by crystallizing the obinutuzumab (GA101) Fab fragment alone and in complex with a CD20 cyclopeptide. Despite recognizing an overlapping epitope, GA101 binds CD20 in a completely different orientation than type I antibodies. Moreover, the elbow angle of GA101 is almost 30° wider than in type I antibodies, potentially resulting in different spatial arrangements of 2 CD20 molecules bound to a single GA101 or rituximab molecule. Using protein tomography, different CD20 complexes were found to be associated with the 2 antibodies, and confocal microscopy showed different membrane compartmentalization of these subpopulations of the cellular CD20 pool. Our findings offer a possible molecular explanation for the different cellular responses elicited by type I and II antibodies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antibodies, Monoclonal / analysis
  • Antibodies, Monoclonal / chemistry
  • Antibodies, Monoclonal / classification*
  • Antibodies, Monoclonal, Humanized
  • Antibodies, Monoclonal, Murine-Derived / chemistry
  • Antibody Specificity
  • Antigens, CD20 / chemistry*
  • Antigens, CD20 / genetics
  • Antigens, CD20 / immunology*
  • Cell Line
  • Crystallography, X-Ray
  • Epitope Mapping / methods
  • Epitopes / analysis
  • Epitopes / chemistry*
  • Humans
  • Models, Molecular
  • Mutagenesis, Site-Directed
  • Protein Structure, Quaternary
  • Protein Structure, Secondary
  • Rituximab

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Antibodies, Monoclonal, Murine-Derived
  • Antigens, CD20
  • Epitopes
  • Rituximab
  • obinutuzumab