核技术
覈技術
핵기술
NUCLEAR TECHNIQUES
2010年
4期
297-302
,共6页
韩彦江%程登峰%张岚%郑明强%周伟%尹端?%武明星%马玉飞%汪勇先
韓彥江%程登峰%張嵐%鄭明彊%週偉%尹耑?%武明星%馬玉飛%汪勇先
한언강%정등봉%장람%정명강%주위%윤단?%무명성%마옥비%왕용선
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
趨化因子%基質細胞衍生因子%N-琥珀酰亞胺-4-氟苯甲痠酯%18F
추화인자%기질세포연생인자%N-호박선아알-4-불분갑산지%18F
Chemokine%Stromal cell-derived factor-1(SDF-1)%SFB%18F
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的一种特异性的拈抗剂.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3 h,放化产率3%(未经衰变校正).
基質細胞衍生因子(SDF-1)及其受體CXCR4在癌癥的髮生和轉移中髮揮著重要作用,因此CXCR4受體可作為診斷癌癥的一箇潛在靶點.多肽T140是趨化因子受體CXCR4的一種特異性的拈抗劑.我們通過閤成中間體[18F]SFB,併和多肽T140的類似物進行偶聯,得到18F標記的CXCR4受體顯像劑多肽[18F]FB-AcTZ14011,併對標記條件進行瞭優化.經過HPLC純化後所得標記多肽的放化純度大于96%,整箇標記用時約3 h,放化產率3%(未經衰變校正).
기질세포연생인자(SDF-1)급기수체CXCR4재암증적발생화전이중발휘착중요작용,인차CXCR4수체가작위진단암증적일개잠재파점.다태T140시추화인자수체CXCR4적일충특이성적념항제.아문통과합성중간체[18F]SFB,병화다태T140적유사물진행우련,득도18F표기적CXCR4수체현상제다태[18F]FB-AcTZ14011,병대표기조건진행료우화.경과HPLC순화후소득표기다태적방화순도대우96%,정개표기용시약3 h,방화산솔3%(미경쇠변교정).
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).
