Combinatorial antibody libraries from cancer patients yield ligand-mimetic Arg-Gly-Asp-containing immunoglobulins that inhibit breast cancer metastasis

Proc Natl Acad Sci U S A. 2004 Dec 7;101(49):17210-5. doi: 10.1073/pnas.0407869101. Epub 2004 Nov 24.

Abstract

Combinatorial antibody libraries have the potential to display the entire immunological record of an individual, allowing one to detect and recover any antibody ever made, irrespective of whether it is currently being produced. We have termed this the "fossil record" of an individual's antibody response. To determine whether cancer patients have ever made antibodies with disease-fighting potential, we screened combinatorial antibody libraries from cancer patients for immunoglobulins that can identify metastatic tumor cells. This strategy yielded human antibodies specific for the activated conformation of the adhesion receptor integrin alphavbeta3 that is associated with a metastatic phenotype. In a remarkable example of convergent evolution, two of these antibodies were shown to contain the Arg-Gly-Asp integrin recognition motif of the natural ligand within the third complementarity-determining region of the heavy chain. These antibodies interfered with lung colonization by human breast cancer cells in a mouse model and inhibited existing metastatic disease. Our data imply that, at least at some time, these antibodies were part of a patient's surveillance system against metastatic cells, targeting the activated conformer of integrin alphavbeta3 and disrupting its functions. The ligand-mimetic nature of these antibodies, combined with specificity for a single receptor, is unique in the integrin-ligand repertoire. The convergent evolution of critical sequences in antibodies and other ligands that bind to the same target means that the immune response has sufficient power to find a best chemical solution for the optimization of binding energy, even though antibodies evolve in real time, as compared with billions of years for the natural ligand.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies, Neoplasm / chemistry
  • Antibodies, Neoplasm / pharmacology
  • Antibodies, Neoplasm / therapeutic use
  • Apoptosis / drug effects
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / immunology
  • Breast Neoplasms / pathology
  • Female
  • Humans
  • Immunoglobulin Fragments / chemistry*
  • Immunoglobulin Fragments / pharmacology
  • Immunoglobulin Fragments / therapeutic use*
  • Integrin alphaVbeta3 / antagonists & inhibitors
  • Integrin alphaVbeta3 / immunology
  • Ligands
  • Lung Neoplasms / prevention & control
  • Lung Neoplasms / secondary
  • Mice
  • Molecular Mimicry
  • Neoplasm Metastasis / drug therapy
  • Neoplasm Metastasis / prevention & control*
  • Neoplasm Transplantation
  • Oligopeptides* / pharmacology
  • Oligopeptides* / therapeutic use
  • Peptide Library*

Substances

  • Antibodies, Neoplasm
  • Immunoglobulin Fragments
  • Integrin alphaVbeta3
  • Ligands
  • Oligopeptides
  • Peptide Library
  • arginyl-glycyl-aspartic acid