Contortrostatin, a snake venom disintegrin with anti-angiogenic and anti-tumor activity

Autor: Fritz Costa, Stephen Swenson, Francis S. Markland, William Ernst, Gary Fujii
Rok vydání: 2006
Předmět:
Zdroj: Pathophysiology of haemostasis and thrombosis. 34(4-5)
ISSN: 1424-8832
Popis: Disintegrins are soluble peptides found in snake venom. They bind to Arg-Gly-Asp (RGD)-responsive integrins with high affinity (nM range) and block integrin function. Contortrostatin (CN), the disintegrin from southern copperhead venom, is a homodimer with a molecular weight of 13,500. Each chain contains 65 amino acids with an Arg-Gly-Asp motif. CN has anti-invasive and anti-adhesive activity on tumor cells and endothelial cells in vitro, and binds to integrins αvβ3, αvβ5, and/or α5β1. In vivo studies using the human metastatic breast cancer cell line MDA-MB-435, in an orthotopic xenograft model in nude mice, revealed that CN has potent anti-tumor and anti-angiogenic activity. Recent studies have employed an intravenous liposomal delivery procedure. Liposomal delivery of CN has also been shown to provide effective in vivo anti-tumor and anti-angiogenic activity in a human ovarian cancer animal model.
Databáze: OpenAIRE