title: Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.
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.
authors.affiliation: CovX Research LLC, 9381 Judicial Drive, Suite 200, San Diego, CA 92130, USA. dvramana@covx.com
authors.forename: Venkata R
authors.initials: VR
authors.lastname: Doppalapudi
authors.forename: Nancy
authors.initials: N
authors.lastname: Tryder
authors.forename: Lingna
authors.initials: L
authors.lastname: Li
authors.forename: Teresa
authors.initials: T
authors.lastname: Aja
authors.forename: David
authors.initials: D
authors.lastname: Griffith
authors.forename: Francesca-Fang
authors.initials: FF
authors.lastname: Liao
authors.forename: Giovanni
authors.initials: G
authors.lastname: Roxas
authors.forename: Mysore P
authors.initials: MP
authors.lastname: Ramprasad
authors.forename: Curt
authors.initials: C
authors.lastname: Bradshaw
authors.forename: Carlos F
authors.initials: CF
authors.lastname: Barbas
mesh_terms: D000818:Animals; D000906:Antibodies / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D065130:Endothelin A Receptor Antagonists; D065131:Endothelin B Receptor Antagonists; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D008819:Mice, Nude; D008968:Molecular Conformation; D009368:Neoplasm Transplantation; D017466:Receptors, Endothelin / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000906:Antibodies; D000970:Antineoplastic Agents; D065130:Endothelin A Receptor Antagonists; D065131:Endothelin B Receptor Antagonists; D007202:Indicators and Reagents; D017466:Receptors, Endothelin