基于促性腺激素释放激素类似物的靶向抗肿瘤化合物研究进展

Targeting drug delivery system based on gonadotropin-releasing hormone analogs: research advances

靶向化疗是一种特异性地将化疗药物靶向到肿瘤部位的治疗方法。由于促性腺激素释放激素(GnRH)受体在大多数肿瘤细胞高表达,而在正常组织或器官上表达很低,因此通过GnRH受体介导的内吞作用将抗癌药物选择性地靶向到肿瘤组织或细胞,可提高抗癌药物的疗效。目前GnRH靶向的载药系统已被广泛研究,极大地提高了药物在肿瘤部位的分布,改善了其水溶性、稳定性,避免产生耐药性,延长了药物在体内的循环时间,使毒副作用明显降低。本文就目前基于GnRH类似物的不同抗癌因子的靶向抗肿瘤药物偶联物进行综述。

Targeted chemotherapy represents a modem oncological strategy designed to specifically deliver the chemotherapeu- tic agents to the tumor site. Gonadotropin-releasing hormone （GnRH） receptor is over-expressed on many types of tumors, and it is present in low or non-detectable quantities in the normal tissues. Thus anti-tumor drugs are specifically delivered to tumor tissues or cells via endocytosis mediated by GnRH receptors and eventually improve its therapeutic efficiency. At present GnRH receptor targeting drug delivery system has been extensively researched, which has greatly increased the drug distribution in tumor sites and improved its stability and solubility and circumvented the development of drug resistance, extended the circulation time in vivo and decreased their peripheral toxicity. This review covers the bioconjugates containing various chemotherapeutic agents, based on GnRH analogs.