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去唾液酸糖蛋白受体介导的肝脏靶向性研究进展
徐文,殷正丰
0
(第二军医大学东方肝胆外科医院分子肿瘤实验室,上海,200438)
摘要:
去唾液酸糖蛋白受体(asialoglycoprotein receptor,ASGPR)又称半乳糖受体,主要表达于哺乳动物肝窦状隙的肝实质细胞表面,参与多种生理功能.多年来ASGPR一直被用于介导药物和基因的肝靶向递送以及肝脏成像等方面的研究,目前已取得许多进展.ASGPR介导的药物肝靶向递送研究主要集中在抗肿瘤药物、降胆固醇药物等.基因肝靶向递送多见于反义药物.肝脏成像研究包括评价肝脏功能、鉴别肝细胞肝癌和肿瘤肝转移灶等.近年来ASGPR的靶向性应用研究还进一步扩展到肝细胞立体培养、肝细胞筛选及肝细胞移植等领域.本文就这些内容作一综述.
关键词:  肝细胞、去唾液酸糖蛋白受体、药物释放系统、基因打靶
DOI:10.3724/SP.J.1008.2006.01002
投稿时间:2006-05-16修订日期:2006-08-21
基金项目:国家重点基础研究发展计划("973"计划)(2002CB523100).
Study on asialoglycoprotein receptor-mediated liver targeting:current progress
XU Wen,YIN Zheng-feng
(第二军医大学东方肝胆外科医院分子肿瘤实验室,上海,200438)
Abstract:
Asialoglycoprotein receptor (ASGPR) , also called galactose receptor, is predominantly expressed on the sinusoidal surface of mammalian hepatocytes and is involved in many physiological functions. For many years ASGPR has been applied for targeting hepatocytes in drug and gene delivery and for functional mapping of the liver, and considerable progress has been made. ASGPR-mediated liver-targeted drug delivery mainly involved anti-tumor drugs and cholesterol-lowering drugs,etc. Liver-targeted gene delivery was often seen in antisense drugs. The research of hepatic imaging mainly involved the evaluation of liver function and identification between hepatocellular carcinoma and hepatic metastasis of tumors. In addition, researchers have also extended its applications to some new fields, such as three-dimension culture of hepatocytes, hepatocytes screening, and hepatocytes transplantation. New achievements in studies of ASGPR-mediated liver targeting are reviewed in this article
Key words:  hepatocytes  asiaglycoprotein receptor  drug delivery systems  gene targeting