首页 / 院系成果 / 成果详情页

Linker effects on biological properties of 111In-Labeled DTPA conjugates of a cyclic RGDfK dimer 期刊论文

编号：

89D5698F656989EA344258335703C053
作者：

Jia, Bing#^[2,3]Liu, Zhaofei(刘昭飞)^[2]Shi, Jiyun^[2,3];Yu, Zilin^[2];Yang, Zhi(杨志)^[4]Zhao, Huiyun^[2];He, Zhengjie^[1];Liu, Shuang*^[1]Wang, Fan(王凡)^[2]
语种：

英文
期刊：

BIOCONJUGATE CHEMISTRY ISSN：1043-1802 2008 年 19 卷 1 期 (201 - 210) ; JAN
收录：
摘要：

In this report, we present in vitro and in vivo evaluation of three In-111-labeled DTPA conjugates of a cyclic RGDfK dimer: DTPA-Bn-SU016 (SU016 = E[c(RGDfK)](2); DTPA-Bn = 2-(p-isothioureidobenzyl)diethylenetriaminepentaacetic acid), DTPA-Bn-E-SU016 (E = glutamic acid) and DTPA-Bn-Cys-SU016 (Cys = cysteic acid). The integrin (43 binding affinities of SU016, DTPA-Bn-SU016, DTPA-Bn-E-SU016, and DTPA-Bn-Cys-SU016 were determined to be 5.0 +/- 0.7 nM, 7.9 +/- 0.6 nM, 5.8 +/- 0.6 nM, and 6.9 +/- 0.9 nM, respectively, against I-125-c(RGDyK) in binding to integrin alpha(v)beta(3), suggesting that E or Cys residue has little effect on the integrin (43 affinity of E[c(RGDfK)12, It was also found that the In-111-labeling efficiency of DTPA-Bn-SU016 and DTPA-Bn-E-SU016 is 3-5 times better than that of DOTA analogues due to fast chelation kinetics and high-yield In-111-labeling under mild conditions (e.g., room temperature). Biodistribution studies were performed using BALB/c nude mice bearing U87MG human glioma xenografts. In-111-DTPA-Bn-SU016, In-111-DTPA-Bn-Cys-SU016, and In-111-DTPA-Bn-Cys-SU016 all displayed rapid blood clearance. Their tumor uptake was comparable between 0.5 and 4 h postinjection (p.i.) within experimental error. (111)InDTPA-Bn-E-SU016 had a significantly lower (p < 0.01) kidney uptake than In-111-DTPA-Bn-SU016 and In-111-DTPA-Bn-Cys-SUO16. The liver uptake of In-111-DTPA-Bn-SU016 was 1.69 +/- 0.18% ID/g at 24 h p.i., while the liver uptake values of In-111-DTPA-Bn-E-SU016 and In-111-DTPA-Bn-Cys-SU016 were 0.55 +/- 0.11% ID/g and 0.79 +/- 0.15% ID/g at 24 h p.i., respectively. Among the three In-111 radiotracers evaluated in this study, In-111-DTPA-Bn-E-SU016 has the lowest liver and kidney uptake and the best tumor/liver and tumor/kidney ratios. Results from metabolism studies indicated that there is little metabolism (<10%) for three In-111 radiotracers at 1 h p.i. Imaging data showed that tumors can be clearly visualized at 4 h p.i. with good contrast in the tumor-bearing mice administered with In-111-DTPA-Bn-E-SU016. It is concluded that using a glutamic acid linker can significantly improve excretion kinetics of the In-labeled E[c(RGDfK)12 from liver and kidneys.
推荐引用方式
GB/T 7714：

Jia Bing,Liu Zhaofei,Shi Jiyun, et al. Linker effects on biological properties of 111In-Labeled DTPA conjugates of a cyclic RGDfK dimer [J].BIOCONJUGATE CHEMISTRY,2008,19(1):201-210.
APA：

Jia Bing,Liu Zhaofei,Shi Jiyun,Yu Zilin,&Wang Fan.(2008).Linker effects on biological properties of 111In-Labeled DTPA conjugates of a cyclic RGDfK dimer .BIOCONJUGATE CHEMISTRY,19(1):201-210.
MLA：

Jia Bing, et al. "Linker effects on biological properties of 111In-Labeled DTPA conjugates of a cyclic RGDfK dimer" .BIOCONJUGATE CHEMISTRY 19,1(2008):201-210.
入库时间：

9/30/2025 4:34:22 PM
更新时间：

9/30/2025 4:34:22 PM

浏览次数：19  下载次数：0

分享到：

浏览次数：19

下载次数：0

打印次数：0