多肽T140类似物的^(18)F标记  

Preparation of ^(18)F-labeled peptide T140 analog

作　　者：韩彦江[1,2] 程登峰[1] 张岚[1] 郑明强[1] 周伟[1] 尹端沚[1] 武明星[1] 马玉飞[1,2] 汪勇先[1] 

机构地区：[1]中国科学院上海应用物理研究所放药中心,上海201800 [2]中国科学院研究生院,北京100049

出　　处：《核技术》2010年第4期297-302,共6页Nuclear Techniques

基　　金：上海市科委(No.06DZ19506);国家自然科学基金(No.20601028)资助

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)。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）.

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 18F 

分 类 号：O615.42[理学—无机化学]