上海交通大学学报（医学版）

›› 2013, Vol. 33 ›› Issue (1): 104-.doi: 10.3969/j.issn.1674-8115.2013.01.021

• 综述 • 上一篇    下一篇

核素标记受体酪氨酸激酶靶向药物显像研究进展

张勰义, 宋少莉, 黄 钢   

  1. 上海交通大学 医学院附属仁济医院核医学科, 上海 200127
  • 出版日期:2013-01-28 发布日期:2013-02-06
  • 通讯作者: 宋少莉, 电子信箱: shaoli-song@163.com；黄 钢, 电子信箱: huang2802@163.com。
  • 作者简介:张勰义（1987—）, 男, 住院医师, 硕士生；电子信箱: rabbitzxy@163.com。
  • 基金资助:

    国家自然科学基金（81101073）；上海市浦江人才计划基金

Research progress of imaging receptor tyrosine kinase targeted drugs by radionuclide

ZHANG Xie-yi, SONG Shao-li, HUANG Gang   

  1. Department of Nuclear Medicine, Renji Hospital, Shanghai Jiaotong University School of Medicine, Shanghai 200127, China
  • Online:2013-01-28 Published:2013-02-06
  • Supported by:

    National Natural Science Foundation of China, 81101073； Shanghai Pujiang Talent Plan

PDF (PC)

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摘要：

跨膜受体酪氨酸激酶信号在肿瘤细胞增殖、抑制凋亡和促进新生血管形成中具有重要作用，多种恶性肿瘤过度表达该受体。随着对受体酪氨酸激酶通路的认知，已设计出众多靶向该靶点的抗肿瘤药物，如单克隆抗体、小分子酪氨酸激酶抑制剂等，临床应用证明这些药物能显著提高抗肿瘤效果，提高患者生存率。但靶向药物靶点专一、价格昂贵，早期监测靶向药物的疗效，对提供临床诊疗决策、减少药物不良反应及节约患者开支具有重要意义。核素标记受体酪氨酸激酶靶向药物显像已用于临床监测靶向药物的疗效，该文就此方面的研究进展进行综述。

关键词: 跨膜酪氨酸激酶受体, 酪氨酸激酶受体, 酪氨酸激酶抑制剂, 核素显像, 反应监测, 靶向药物

Abstract:

Transmembrane receptor tyrosine kinase signalling triggers cell proliferation, apoptosis suppression and neovasculature recruitment. Transmembrane receptor tyrosine kinases are overexpressed in many malignancies, which have become the molecular targets for an increasing number of anticancer drugs. For example, monoclonal antibodies and small-molecule tyrosine kinase inhibitors have been clinically proved to boost the therapeutic effect and increase the survival of patients. However, the targeted drugs are clinically limited by specific target and high price, and the early monitoring of therapeutic effects of targeted drugs is important for the design of clinical regimen and reduction of adverse effects and medical expense. The imaging of receptor tyrosine kinase targeted drugs by radionuclide has been clinically employed in the monitoring of therapeutic effects of targeted drugs, and the research progress of this application is reviewed in this paper.

Key words: transmembrane receptor tyrosine kinases, receptor tyrosine kinases, tyrosine kinase inhibitors, radionuclide, response monitor, targeted drugs