Retro-Inverso Carbohydrate Mimetic Peptides with Annexin1-Binding Selectivity, Are Stable In Vivo, and Target Tumor Vasculature
Retro-Inverso Carbohydrate Mimetic Peptides with Annexin1-Binding Selectivity, Are Stable In Vivo, and Target Tumor Vasculature
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DOI：
10.1371/journal.pone.0080390
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发表时间：
2013-12-02
期刊：
影响因子：
3.7
通讯作者：
Sha, Xianyi
中科院分区：
文献类型：
--
作者：
Chen, Xinyi;Fan, Zhuoyang;Sha, Xianyi
先前的研究表明，碳水化合物模拟肽IF 7（IFLLWQR）对肿瘤内皮上的特异性标记物膜联蛋白1（Anxa 1）具有出色的靶向特性。然而，IF7对蛋白水解敏感并且在体内具有差的稳定性。我们制备了一种D-氨基酸，IF7的反向序列肽，命名为RIF7，以赋予蛋白酶抗性，同时保留生物活性。实验结果表明，RIF7具有显着增加的稳定性和增加的受体结合亲和力比IF7，这种新的部分可能代表抗癌药物的临床相关的车辆。
Previous research suggests that carbohydrate mimetic peptide IF7 (IFLLWQR) has an excellent targeting property to annexin1 (Anxa1), a specific marker on the tumor endothelium. However, IF7 is susceptible to proteolysis and has a poor stability in vivo. We prepared a D-amino acid, reverse sequence peptide of IF7, designated RIF7, to confer protease resistance while retaining bioactivity. Experimental results indicate that RIF7 had significantly increased stability and an increased receptor binding affinity than IF7, and this new moiety may represent a clinically relevant vehicle for anticancer drugs.