Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.

  title={Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.},
  author={Venkata Ramana Doppalapudi and Nancy Tryder and Lingna Li and Teresa Aja and David Griffith and F Liao and Giovanni Roxas and Mysore P. Ramprasad and Curt Bradshaw and Carlos F. Barbas},
  journal={Bioorganic & medicinal chemistry letters},
  volume={17 2},
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. 

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