Cornelissen Bart, Vallis Katherine A
MRC/CRUK Gray Institute for Radiation Oncology and Biology, University of Oxford, Oxford, OX3 7LJ, UK.
Curr Drug Discov Technol. 2010 Dec;7(4):263-79. doi: 10.2174/157016310793360657.
The review presented here lays out the present state of the art in the field of radionuclide therapies specifically targeted against the nucleus of cancer cells, focussing on the use of Auger-electron-emitters. Nuclear localisation of radionuclides increases DNA damage and cell kill, and, in the case of Auger-electron therapy, is deemed necessary for therapeutic effect. Several strategies will be discussed to direct radionuclides to the nucleoplasm, even to specific protein targets within the nucleus. An overview is given of the applications of Auger-electron-emitting radionuclide therapy targeting the nucleus. Finally, a few suggestions are made as how radioimmunotherapy with nuclear targets can be improved, and the challenges that might be met, such as how to perform accurate dosimetry measurements, are examined.
本文所呈现的综述阐述了放射性核素疗法领域的当前技术水平，该疗法专门针对癌细胞的细胞核，重点关注俄歇电子发射体的应用。放射性核素的核定位会增加DNA损伤和细胞杀伤，并且在俄歇电子疗法中，被认为对治疗效果是必要的。将讨论几种将放射性核素导向核质甚至细胞核内特定蛋白质靶点的策略。概述了靶向细胞核的俄歇电子发射放射性核素疗法的应用。最后，就如何改进针对核靶点的放射免疫疗法提出了一些建议，并探讨了可能遇到的挑战，例如如何进行精确的剂量测定。
