Cross-domain inhibition of TACE ectodomain

Proc Natl Acad Sci U S A. 2011 Apr 5;108(14):5578-83. doi: 10.1073/pnas.1017067108. Epub 2011 Mar 17.

Abstract

Proteolytic release from the cell surface is an essential activation event for many growth factors and cytokines. TNF-α converting enzyme (TACE) is a membrane-bound metalloprotease responsible for solubilizing many pathologically significant membrane substrates and is an attractive therapeutic target for the treatment of cancer and arthritis. Prior attempts to antagonize cell-surface TACE activity have focused on small-molecule inhibition of the metalloprotease active site. Given the highly conserved nature of metalloprotease active sites, this paradigm has failed to produce a truly specific TACE inhibitor and continues to obstruct the clinical investigation of TACE activity. We report the bespoke development of a specific TACE inhibitory human antibody using "two-step" phage display. This approach combines calculated selection conditions with antibody variable-domain exchange to direct individual antibody variable domains to desired epitopes. The resulting "cross-domain" human antibody is a previously undescribed selective TACE antagonist and provides a unique alternative to small-molecule metalloprotease inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ADAM Proteins / antagonists & inhibitors*
  • ADAM Proteins / metabolism
  • ADAM17 Protein
  • Animals
  • Antibodies / pharmacology*
  • Drug Design*
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Immunoglobulin Variable Region / genetics
  • Immunoglobulin Variable Region / metabolism*
  • Mice
  • Models, Molecular*
  • Mutagenesis
  • Peptide Library
  • Protein Structure, Tertiary / genetics
  • Surface Plasmon Resonance

Substances

  • Antibodies
  • Immunoglobulin Variable Region
  • Peptide Library
  • ADAM Proteins
  • ADAM17 Protein
  • ADAM17 protein, human
  • Adam17 protein, mouse