论文部分内容阅读
Integrin-targeting has been shown to be an effective approach for anti-cancer/anti-angiogenic therapy.Disintegrins are peptides originally isolated from snake venom that avidly attach to human integrins, including αvβ3/αtvβ5/α5β1.The Arg-Gly-Asp (RGD)-disintegrin isolated from southern copperhead venom, contortrostatin (CN), was shown to be a highly effective anti-cancer agent in several animal models of cancer.Although the pharmacological properties of CN made it an intriguing molecule for anti-cancer therapy, only limited quantities are available in venom.Therefore, we have developed a recombinant expression system that allowed us to prepare large quantities of a modified version of the venom disintegrin, which we call vicrostatin (VCN).VCN retains the same bioactivity as CN and binds to integrins involved in tumor invasion and metastasis;it is a potent anti-angiogenic agent in murine models of human cancer.