Macklis R M, Kinsey B M, Kassis A I, Ferrara J L, Atcher R W, Hines J J, Coleman C N, Adelstein S J, Burakoff S J
Joint Center for Radiation Therapy, Harvard Medical School, Boston, MA 02115.
Science. 1988 May 20;240(4855):1024-6. doi: 10.1126/science.2897133.
Alpha particles are energetic short-range ions whose higher linear energy transfer produces extreme cytotoxicity. An alpha-particle-emitting radioimmunoconjugate consisting of a bismuth-212-labeled monoclonal immunoglobulin M specific for the murine T cell/neuroectodermal surface antigen Thy 1.2 was prepared. Analysis in vitro showed that the radioimmunoconjugate was selectively cytotoxic to a Thy 1.2+ EL-4 murine tumor cell line. Approximately three bismuth-212-labeled immunoconjugates per target cell reduced the uptake of [3H]thymidine by the EL-4 target cells to background levels. Mice inoculated intraperitoneally with EL-4 cells were cured of their ascites after intraperitoneal injection of 150 microcuries of the antigen-specific radioimmunoconjugate, suggesting a possible role for such conjugates in intracavitary cancer therapy.
α粒子是具有高能量的短程离子，其较高的线性能量传递会产生极强的细胞毒性。制备了一种发射α粒子的放射免疫偶联物，它由针对小鼠T细胞/神经外胚层表面抗原Thy 1.2的铋-212标记的单克隆免疫球蛋白M组成。体外分析表明，该放射免疫偶联物对Thy 1.2+ EL-4小鼠肿瘤细胞系具有选择性细胞毒性。每个靶细胞大约三个铋-212标记的免疫偶联物可将EL-4靶细胞对[3H]胸腺嘧啶核苷的摄取降低至背景水平。腹腔注射EL-4细胞的小鼠在腹腔注射150微居里的抗原特异性放射免疫偶联物后，腹水得以治愈，这表明此类偶联物在腔内癌症治疗中可能具有一定作用。
