Targeted drug delivery to tumor endothelial surface.

在以前发现的碳水化合物模拟多肽中，我们发现了一种多肽(Proc Natl Acad Sci USA)。2009)，命名为IF7，与高度特异的肿瘤内皮细胞表面标志Annexin 1(Anxa1)结合。合成的IF7多肽与荧光Alexa 488偶联后，在静脉注射后几分钟内靶向肿瘤，该靶向可被抗Anxa1抗体抑制。与抗癌药物偶联的IF7被静脉注射到携带人类癌细胞产生的荧光素酶阳性肿瘤的裸鼠体内。IVIS[0！R]Living 3D图像系统显示，IF7-抗癌药物治疗实质上抑制了肿瘤的生长，但在某些情况下肿瘤消失了。IF7-抗癌药物在低剂量下有效，药物治疗后小鼠无明显副作用。鉴于其极其特异的肿瘤靶向活性，IF7因此是一种具有临床意义的抗癌药物载体。

Among previously identified carbohydrate-mimicry peptides, we found one peptide (Proc Natl Acad Sci USA. 2009), designated as IF7, binds to Annexin 1 (Anxa1), a highly specific tumor endothelial cell surface marker. A synthetic IF7 peptide conjugated with fluorescent Alexa 488 targeted the tumor within several minutes of intravenous injection, which was inhibited by anti-Anxa1 antibody. IF7 conjugated with the anti-cancer drug was injected intravenously into nude mice carrying luciferase-positive tumors produced by human cancer cells. IVIS[○!R] Living 3D Image System showed that IF7-anticancer drug treatment substantially suppressed tumor growth, while in some cases the tumor disappeared. IF7-anticancer drug was effective at low dosages, and mice showed no apparent side effects following drug treatment. Given its extremely specific tumor-targeting activity, IF7 therefore represent a clinically relevant vehicle for anticancer drugs.