Chemically programmed antibodies: Endothelin receptor targeting CovX-Bodies™

Autor:	Teresa Aja, Giovanni Roxas, Nancy Tryder, Carlos F. Barbas, Curt Bradshaw, Mysore P. Ramprasad, Francesca Fang Liao, Lingna Li, David A. Griffith, Venkata Doppalapudi
Rok vydání:	2007
Předmět:	Endothelin A Receptor Antagonists medicine.drug_class Clinical Biochemistry Lysine Molecular Conformation Mice Nude Pharmaceutical Science Antineoplastic Agents CHO Cells Monoclonal antibody Biochemistry Antibodies Mice Structure-Activity Relationship Cricetulus In vivo Cricetinae Drug Discovery medicine Animals Humans Molecular Biology Receptors Endothelin Chemistry Organic Chemistry Biological activity Small molecule In vitro Endothelin B Receptor Antagonists Cell culture Molecular Medicine Indicators and Reagents Endothelin receptor Neoplasm Transplantation
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:501-506
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::004f3f7faa5d353622e71914c9200338 https://doi.org/10.1016/j.bmcl.2006.10.009 Zobrazit plný text záznamu Full Text from ScienceDirect