以整合素αvβ3为靶点的肿瘤靶向制剂

Integrin αvβ3 Targeting RGD-Peptidomimetic Agents

整合素αvβ3在肿瘤细胞及肿瘤血管内皮细胞中高表达,RGD序列作为其配体,可与其进行特异性结合,为肿瘤的诊断和靶向治疗提供了理论基础。RGD诊断试剂的前期研究和临床试验数据表明其具有良好的肿瘤组织靶向性。RGD-纳米抗肿瘤制剂(RGD-脂质体、RGD-胶束和RGD-纳米粒)在体外可提高细胞对药物的吸收率,增强细胞毒性;在动物移植瘤模型中,能更好地抑制肿瘤的生长,延长了动物的生存时间。在肿瘤发病率居高不下,治疗手段和疗效都较为有限的今天,RGD靶向制剂在肿瘤诊断和治疗中所具有的优势值得特别关注。

As RGD can specifically bind to integrin αvβ3, which is up-regulated in both tumor and tumor-en-dothelial cells, this enables the targeting of diagnostics and therapeutics of tumor using the affinity between RGD and its receptor. Previous studies and data from clinical trials demonstrated RGD imaging agents can target tumor tissues. RGD-nano antitumor agents（RGD-liposome, RGD-micelle, RGD-nanoparticle） have greater cellular uptake and higher cytotoxic in vitro, make more effective in tumor growth inhibition and prolong survival times in xeno-graft models. Tumor incidence increases year by year, but therapeutics and efficacy are still very limited. The ad-vantage of RGD-peptidomimetic agents in targeting of diagnostics and therapeutics deserve special attention.