Author/Authors :
Venkata R. Doppalapudi، نويسنده , , Nancy Tryder، نويسنده , , Lingna Li، نويسنده , , Teresa Aja، نويسنده , , David Griffith، نويسنده , , Francesca-Fang Liao، نويسنده , , Giovanni Roxas، نويسنده , , Mysore P. Ramprasad، نويسنده , , Curt Bradshaw، نويسنده , , Carlos F. Barbas III، نويسنده ,
Abstract :
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.
Keywords :
Monoclonal antibodies , Aldolase antibody , Endothelin-A , CovX-Body™ , Endothelin-A (ETA) antagonists , Antitumor efficacy