Contortrostatin, a snake venom disintegrin with anti-angiogenic and anti-tumor activity.
Contortrostatin, a snake venom disintegrin with anti-angiogenic and anti-tumor activity.
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Contortrostatin，一种蛇毒解整合素，具有抗血管生成和抗肿瘤活性。
DOI：
10.1159/000092418
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发表时间：
2005
期刊：
影响因子：
--
通讯作者：
Markland,FrancisS
中科院分区：
文献类型：
--
作者：
Swenson,Stephen;Costa,Fritz;Ernst,William;Fujii,Gary;Markland,FrancisS
解整合素是在蛇毒中发现的可溶性肽。它们以高亲和力 (nMrange) 与 Arg-Gly-Asp (RGD) 响应性整合素结合并阻断整合素功能。 Contortrostatin (CN) 是来自南方铜头蛇毒液的解整合素，是一种同型二聚体，分子量为 13,500。每条链包含 65 个氨基酸，带有 Arg-Gly-Asp 基序。 CN 在体外对肿瘤细胞和内皮细胞具有抗侵袭和抗粘附活性，并与整合素 αvβ3、αvβ5 和/或 α5β1 结合。在裸鼠原位异种移植模型中使用人转移性乳腺癌细胞系 MDA-MB-435 进行的体内研究表明，CN 具有有效的抗肿瘤和抗血管生成活性。最近的研究采用了静脉内脂质体递送程序。 CN 的脂质体递送也已被证明在人卵巢癌动物模型中提供有效的体内抗肿瘤和抗血管生成活性。
Disintegrins are soluble peptides found in snake venom. They bind to Arg-Gly-Asp (RGD)-responsive integrins with high affinity (nMrange) 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.