高等学校化学学报 ›› 2013, Vol. 34 ›› Issue (4): 870.doi: 10.7503/cjcu20120995

• 生物化学 • 上一篇    下一篇

利用噬菌体展示技术筛选放射性标记肺癌靶肽YC11及其生物分布

梁坤, 褚泰伟   

  1. 北京分子科学国家实验室, 北京大学化学与分子工程学院应用化学系, 北京 100871
  • 收稿日期:2012-11-02 出版日期:2013-04-10 发布日期:2013-03-21
  • 通讯作者: 褚泰伟,男,博士,副教授,主要从事放射性药物化学方面的研究.E-mail:twchu@pku.edu.cn E-mail:twchu@pku.edu.cn
  • 基金资助:

    国家自然科学基金(批准号:21071010)资助.

Screening, Radiolabeling and Biodistribution of Lung Tumor-targeting Peptide YC11 by in vivo Phage Display

LIANG Kun, CHU Tai-Wei   

  1. Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
  • Received:2012-11-02 Online:2013-04-10 Published:2013-03-21

摘要:

利用体内噬菌体展示技术筛选了肿瘤特异性结合靶肽, 获得了肺腺癌靶肽CSIHYPLSC(YC11)并对其进行了放射性碘标记. 采用反相高效液相色谱技术(RP-HPLC)分离纯化131I-YC11和对照肽131I-NGR, 放化纯度大于99%. 在荷人肺腺癌A549裸鼠体内的分布结果表明, 131I-YC11的肿瘤/血液放射性计数比为0.62, 肿瘤/心脏放射性计数比为2.06, 肿瘤/肺放射性计数比为1.11, 肿瘤/肝脏放射性计数比为0.81, 略高于131I-NGR的对应值. 131I-YC11在肿瘤中的摄取值为2.79%ID/g, 与131I-NGR在肿瘤中的摄取值(1.61%ID/g)相比, 131I-YC11的肿瘤摄取高于多肽131I-NGR.

关键词: 噬菌体展示, 靶肽, 肺癌, 生物分布, 放射性标记

Abstract:

In vivo phage display was used to isolate tumor-targeting peptides. A cycloheptapeptide CSIHYPLSC(YC11) ligand targeting A549 human lung tumor was identified and radioiodinated. The labeled complex 131I-YC11 and 131I-NGR(control peptide) were isolated and purified by reverse phase high-performance liquid chromatography(RP-HPLC). The radiochemical purity was estimated to be better than 99%. The biodistribution results of 131I-YC11 and control peptide 131I-NGR in mice bearing A549 tumor demonstrated that the tumor-to-blood, tumor-to-heart, tumor-to-lung and tumor-to-liver uptake ratios of 131I-YC11 were 0.62, 2.06, 1.11 and 0.81, respectively, and slightly higher than those of 131I-NGR. The uptake of 131I-YC11 in tumor was 2.79%ID/g, more than that of 131I-NGR(1.61%ID/g). 131I-YC11 was more concentrated in A549 tumor than 131I-NGR. Conclusively, YC11 could be a potential lung cancer targeting agent.

Key words: Phage display, Targeting peptide, Lung tumor, Biodistribution, Radiolabeling

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