Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, Villigen-PSI, Switzerland.
J Nucl Med. 2011 Jan;52(1):1-4. doi: 10.2967/jnumed.110.076018. Epub 2010 Dec 13.
The folate receptor (FR) is overexpressed on a variety of tumor types, whereas its distribution in normal tissues and organs is highly limited. Exploration of the utility of the FR revealed its promising potential for targeting with folate-based radiopharmaceuticals. Herein, we report the principle of the FR-targeting strategy and summarize the development of several folic acid radioconjugates useful for SPECT and PET of cancer diseases. The potential applicability of folate radiopharmaceuticals for FR-targeted radionuclide therapy is also discussed.
叶酸受体 (FR) 在多种肿瘤类型中过表达，而在正常组织和器官中的分布则受到高度限制。对 FR 应用价值的探索揭示了其在基于叶酸的放射性药物靶向方面的巨大潜力。本文报告了 FR 靶向策略的原理，并总结了几种用于癌症疾病 SPECT 和 PET 的叶酸放射性药物偶联物的发展情况。还讨论了叶酸放射性药物在 FR 靶向放射性核素治疗中的潜在适用性。
