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多肽T140类似物的~(18)F标记
引用本文:韩彦江,程登峰,张岚,郑明强,周伟,尹端?,武明星,马玉飞,汪勇先.多肽T140类似物的~(18)F标记[J].核技术,2010,33(4).
作者姓名:韩彦江  程登峰  张岚  郑明强  周伟  尹端?  武明星  马玉飞  汪勇先
作者单位:1. 中国科学院上海应用物理研究所放药中心,上海,201800;中国科学院研究生院,北京,100049
2. 中国科学院上海应用物理研究所放药中心,上海,201800
基金项目:上海市科委项目,国家自然科学基金 
摘    要:基质细胞衍生因子(SDF-1)及其受体CXCR4在癌症的发生和转移中发挥着重要作用,因此CXCR4受体可作为诊断癌症的一个潜在靶点。多肽T140是趋化因子受体CXCR4的一种特异性的拮抗剂。我们通过合成中间体18F]SFB,并和多肽T140的类似物进行偶联,得到18F标记的CXCR4受体显像剂多肽18F]FB-AcTZ14011,并对标记条件进行了优化。经过HPLC纯化后所得标记多肽的放化纯度大于96%,整个标记用时约3h,放化产率3%(未经衰变校正)。

关 键 词:趋化因子  基质细胞衍生因子  N-琥珀酰亚胺-4-氟苯甲酸酯

Preparation of 18F-labeled peptide T140 analog
HAN Yanjiang,CHENG Dengfeng,ZHANG Lan,ZHENG Mingqiang,ZHOU Wei,YIN Duanzhi,WU Mingxing,MA Yufei,WANG Yongxian.Preparation of 18F-labeled peptide T140 analog[J].Nuclear Techniques,2010,33(4).
Authors:HAN Yanjiang  CHENG Dengfeng  ZHANG Lan  ZHENG Mingqiang  ZHOU Wei  YIN Duanzhi  WU Mingxing  MA Yufei  WANG Yongxian
Abstract:Stromal cell-derived factor-1 (SDF-1) and its receptor CXCR4 play an important role in the carcinogenesis and metastasis of tumors. CXCR4 can be a potential target for the in vivo imaging of tumors. T140 is a specific antagonist of chemokine receptor CXCR4. By optimizing the reaction parameters, a peptide ligand of CXCR4, 18F]FB-AcTZ14011 was prepared through 18F labeled prosthetic group 18F]SFB and coupled with the analog of the peptide T140. After HPLC purification, radiochemical purity of the labeled peptide was more than 96%, and 18F]FB-AcTZ14011 was produced in 3 h with a radiochemical yield of 3% (without decay-correction).
Keywords:18F  Chemokine  Stromal cell-derived factor-1(SDF-1)  SFB  18F
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