Li Yan Michael, Vallera Daniel A, Hall Walter A
Department of Neurosurgery, State University of New York Upstate Medical University, Syracuse, NY 13210, USA.
J Neurooncol. 2013 Sep;114(2):155-64. doi: 10.1007/s11060-013-1157-8. Epub 2013 May 22.
Targeted toxins (TT) are molecules that bind cell surface antigens or receptors such as the transferrin or interleukin-13 receptor that are overexpressed in cancer. After internalization, the toxin component kills the cell. These recombinant proteins consist of an antibody or carrier ligand coupled to a modified plant or bacterial toxin such as diphtheria toxin (DT). These fusion proteins are very effective against brain cancer cells that are resistant to radiation therapy and chemotherapy. TT have shown an acceptable profile for toxicity and safety in animal studies and early clinical trials have demonstrated a therapeutic response. This review summarizes the characteristics of DT-based TT, the animal studies in malignant brain tumors and early clinical trial results. Obstacles to the successful treatment of brain tumors include poor penetration into tumor, the immune response to DT and cancer heterogeneity.
靶向毒素(TT)是一类能够结合细胞表面抗原或受体的分子,如在癌症中过度表达的转铁蛋白或白细胞介素-13受体。内化后,毒素成分会杀死细胞。这些重组蛋白由与修饰的植物或细菌毒素(如白喉毒素(DT))偶联的抗体或载体配体组成。这些融合蛋白对抵抗放射治疗和化疗的脑癌细胞非常有效。在动物研究中,TT已显示出可接受的毒性和安全性特征,早期临床试验也证明了其治疗效果。本综述总结了基于DT的TT的特性、在恶性脑肿瘤中的动物研究以及早期临床试验结果。脑肿瘤成功治疗的障碍包括对肿瘤的穿透性差、对DT的免疫反应以及癌症异质性。