摘要
叶酸受体(FR)在肿瘤细胞表面过度表达,而在正常细胞中则几乎不表达或微量表达。叶酸受体可作为靶点用于肿瘤识别和抗癌药靶向投递。然而,叶酸和叶酸结合物对FR-α和FR-β亚型结合能力相似,且这两种主要的FR亚型可同时在生物中表达,造成叶酸对肿瘤组织或炎症区域不能选择性地靶向治疗和成像。因此,研究FR亚型与叶酸及其类似物特异性结合关系将对提高癌症识别特异性和抗癌药靶向投递效率具有重要意义。本文阐述了FR亚型在肿瘤组织的分布特性,与配体特异性作用机制,介绍了近几年来FR亚型介导的肿瘤靶向光学成像技术和肿瘤靶向治疗技术的研究进展。指出了当前研究存在的问题和今后发展的方向。
Folate receptor （FR） is over-expressed on the sion on normal cells, so FR could be exploited as target epithelial of the tumor cells, while limited expres spot to recognize tumour and target delivery anti cancer drugs. However, folate and its conjugates have a parallel combining capacity with FR-α and FR-β, the two major FR-isoform expressed in vivo simultaneous, which made that folate can not be selectivity used for targeted therapy and imaging to malignant tissue or inflammation. So studying specific bonding re- lationship between FR-isoform and folate （or its analogue） has a significance to improve cancer recognition specificity and efficiency of anti-cancer drugs targeting the delivery. In this paper, distribution characteris- tics of the FR-isoform in tumor tissue and its mechanism on the binding specific ligand are described. Re- search progress of FR-isoform mediated tumor targeting optical imaging and targeting cure technology in re- cent years are also summarized. The problems in current research and future prospects are also proposed in this review.
出处
《中国科学基金》
CSSCI
CSCD
北大核心
2014年第1期26-31,共6页
Bulletin of National Natural Science Foundation of China
关键词
叶酸受体
亚型
肿瘤
高效介导
肿瘤成像
靶向治疗
Folate receptor, isoform
tumour, efficient mediation, tumor imaging, targeting therapy
