- Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.
Bioorganic & medicinal chemistry letters (2006-10-24)
Venkata R Doppalapudi, Nancy Tryder, Lingna Li, Teresa Aja, David Griffith, Francesca-Fang Liao, Giovanni Roxas, Mysore P Ramprasad, Curt Bradshaw, Carlos F Barbas
PMID17055724
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.
MATERIALS