Targeted therapy using alpha emitters.
Targeted therapy using alpha emitters.
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使用阿尔法发射器进行靶向治疗。
DOI：
10.1088/0031-9155/41/10/005
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发表时间：
1996
影响因子：
3.5
通讯作者：
Zalutsky,MR
中科院分区：
文献类型：
--
作者：
Vaidyanathan,G;Zalutsky,MR
放射性核素，例如通过发射粒子而衰变的和，对于靶向放射疗法的某些应用是有吸引力的。和粒子的组织穿透仅相当于几个细胞直径，提供了将细胞特异性靶向与类似范围的辐射相结合的可能性。与放射性核素（如和）发射的粒子不同，粒子是高线性能量转移的辐射，因此具有更大的生物效力。已经探索了几种用于靶向放射治疗的方法，所述靶向放射治疗使用标记物质，包括胶体、单克隆抗体、代谢前体、亲受体配体和其他低分子量分子。另一种使发射放射性药物的前景更加光明的试剂是Meta-[]阿司他托苄基胍。在单细胞条件下，通过[]胸苷掺入和有限稀释克隆形成试验测定，该化合物对人神经母细胞瘤细胞的毒性比Meta-[]碘苄胍高1000倍。对于Meta-[]阿司他基苄基胍，该值相当于每个细胞仅结合原子。这些结果提示Meta-[]阿司他丁苄胍可能是微转移性神经母细胞瘤靶向放射治疗的一种有价值的药物。
Radionuclides such as and which decay by the emission of-particles are attractive for certain applications of targeted radiotherapy. The tissue penetration of and-particles is equivalent to only a few cell diameters, offering the possibility of combining cell-specific targeting with radiation of similar range. Unlike the-particles emitted by radionuclides such as and,-particles are radiation of high linear energy transfer and thus greater biological effectiveness. Several approaches have been explored for targeted radiotherapy with-and-labelled substances including colloids, monoclonal antibodies, metabolic precursors, receptor-avid ligands and other lower molecular weight molecules. An additional agent which exemplifies the promise of-emitting radiopharmaceuticals is meta-[] astatobenzylguanidine. The toxicity of this compound under single-cell conditions, determined both by [] thymidine incorporation and by limiting dilution clonogenic assays, for human neuroblastoma cells is of the order of 1000 times higher than that of meta-[] iodobenzylguanidine. For meta-[] astatobenzylguanidine, the value was equivalent to only atoms bound per cell. These results suggest that meta-[] astatobenzylguanidine might be valuable for the targeted radiotherapy of micrometastatic neuroblastomas.