叶酸在放射性核素标记研究中的应用

Recent Progress in Application of Folate in Radionuclide Labeling

叶酸在人体内有重要的生理功能,它能特异性结合过度表达于许多肿瘤(卵巢癌、乳腺癌、直肠癌等)细胞膜表面的叶酸受体。在肿瘤靶向药物输运体系中,包括输运放射性核素标记的叶酸螯合物显像剂,叶酸受体是一种潜在的分子靶。近年来,有关放射性核素标记的叶酸螯合物显像剂的研究越来越多。本文着重介绍了放射性核素111In6、7Ga和99Tcm(Re)标记叶酸的螯合物显像剂以及它们在肿瘤诊断方面的临床应用。这些资料表明,99Tcm标记叶酸的螯合物是一种比较有发展前途的显像剂。

The folate receptor is known to be overexpressed by a variety of neoplastic tissues, including ovrian, breast, colorectal and other human tumors. It is a potential molecular target for tumor-selective drug delivery, including delivery of radiolabeled folate-chelate conjugates for diagnostic imaging. Recently, the growing study on tumor imaging with radionuclide agents targeted to the folate receptor are more and more, but this review mainly concentrated on the clinical application of ^111In,^67Ga and ^99Tc^m （Re） labeling folate-chelate conjugates in tumor diagnostic imaging. However, these existing data shows that the ^99Tc^m （Re） labeling folate-chelate conjugate is a good folate receptor imaging agent.