Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies

Bioorg Med Chem Lett. 2007 Jan 15;17(2):501-6. doi: 10.1016/j.bmcl.2006.10.009. Epub 2006 Oct 7.


Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.

MeSH terms

  • Animals
  • Antibodies / chemistry*
  • Antibodies / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Endothelin A Receptor Antagonists
  • Endothelin B Receptor Antagonists
  • Humans
  • Indicators and Reagents
  • Mice
  • Mice, Nude
  • Molecular Conformation
  • Neoplasm Transplantation
  • Receptors, Endothelin / drug effects*
  • Structure-Activity Relationship


  • Antibodies
  • Antineoplastic Agents
  • Endothelin A Receptor Antagonists
  • Endothelin B Receptor Antagonists
  • Indicators and Reagents
  • Receptors, Endothelin