叶酸受体介导的肿瘤细胞靶向分子显像剂的研究进展

Progress of targeted diagnostic imaging agents on cancer mediated folate-receptor

叶酸受体在肿瘤细胞中都有过度表达,通过其介导细胞内化能够将叶酸摄取入细胞浆内,因此利用叶酸受体与叶酸及其类似物偶联的分子显像剂特异性结合,可以达到肿瘤组织靶向分布和显像目的,在肿瘤诊断和治疗方面很有前景。本文根据近年来的文献资料,对叶酸受体介导的靶向分子显像剂的研究进展作了概述。

The folate receptor （FR） is an over-expressed tumor-associated antigen that binds folate and folate-drug conjugates with very high affinity and shuttles these bound molecules inside cells via an endoeytic mechanism. Using folic acid as a targeting ligand ,a variety of imaging agents can be delivered to FR-positive cells. As such,this review will outline the manner in which folate - drug conjugates are screened preclinically, it will highlight the various methods for diagnostic and therapeutic imaging that are currently under investigation.