The imaging of insulinomas using a radionuclide-labelled molecule of the GLP-1 analogue liraglutide: a new application of liraglutide.
The imaging of insulinomas using a radionuclide-labelled molecule of the GLP-1 analogue liraglutide: a new application of liraglutide.
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使用 GLP-1 类似物利拉鲁肽的放射性核素标记分子对胰岛素瘤进行成像：利拉鲁肽的新应用。
DOI：
10.1371/journal.pone.0096833
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发表时间：
2014
期刊：
影响因子：
3.7
通讯作者：
Zhang Y
中科院分区：
文献类型：
--
作者：
Lv J;Pan Y;Li X;Cheng D;Liu S;Shi H;Zhang Y
本研究通过对125i标记的胰高血糖素样肽-1 （GLP-1）类似物利拉鲁肽用于胰岛素瘤体内和体外小动物SPECT/CT（单光子发射计算机断层扫描/计算机断层扫描）成像的初步研究，探索了一种新的非侵入性成像方法，用于胰岛素瘤的特异性诊断。利拉鲁肽碘碘标记125I。然后将标记的125i -利拉鲁肽化合物与来自INS-1细胞系的胰岛素瘤细胞进行体外饱和和竞争结合实验。此外，在裸鼠模型中，使用125i -利拉鲁肽对胰岛素瘤进行体内小动物SPECT/CT成像，并检查其在各器官中的放射性分布。用125I标记利拉鲁肽是成功的，标记率约为95%，放射化学纯度大于95%。125i -利拉鲁肽与ns -1细胞表面GLP-1受体结合的平衡解离常数（Kd）为128.8±30.4 nmol/L(N = 3)，半抑制浓度（IC50）为542.4±187.5 nmol/L（N = 3）。125i -利拉鲁肽小动物SPECT/CT显像显示，125i -利拉鲁肽治疗后90 min肿瘤显像最清晰。体内放射性分布检测显示，125i -利拉鲁肽治疗90 min后，肿瘤和肌肉组织的靶/非靶（T/NT）比为4.83±1.30（N = 3）。我们的研究表明125i -利拉鲁肽主要被肝脏和肾脏代谢和清除。放射性核素125i -利拉鲁肽可用于胰岛素瘤的特异性成像，为胰岛素瘤的体内诊断提供了一种新的无创方法。
This study explores a new, non-invasive imaging method for the specific diagnosis of insulinoma by providing an initial investigation of the use of 125I-labelled molecules of the glucagon-like peptide-1 (GLP-1) analogue liraglutide for in vivo and in vitro small-animal SPECT/CT (single-photon emission computed tomography/computed tomography) imaging of insulinomas. Liraglutide was labelled with 125I by the Iodogen method. The labelled 125I-liraglutide compound and insulinoma cells from the INS-1 cell line were then used for in vitro saturation and competitive binding experiments. In addition, in a nude mouse model, the use of 125I-liraglutide for the in vivo small-animal SPECT/CT imaging of insulinomas and the resulting distribution of radioactivity across various organs were examined. The labelling of liraglutide with 125I was successful, yielding a labelling rate of approximately 95% and a radiochemical purity of greater than 95%. For the binding between 125I-liraglutide and the GLP-1 receptor on the surface of INS-1 cells, the equilibrium dissociation constant (Kd) was 128.8±30.4 nmol/L(N = 3), and the half-inhibition concentration (IC50) was 542.4±187.5 nmol/L(N = 3). Small-animal SPECT/CT imaging with 125I-liraglutide indicated that the tumour imaging was clearest at 90 min after the 125I-liraglutide treatment. An examination of the in vivo distribution of radioactivity revealed that at 90 min after the 125I-liraglutide treatment, the target/non-target (T/NT) ratio for tumour and muscle tissue was 4.83±1.30(N = 3). Our study suggested that 125I-liraglutide was predominantly metabolised and cleared by the liver and kidneys. The radionuclide 125I-liraglutide can be utilised for the specific imaging of insulinomas, representing a new non-invasive approach for the in vivo diagnosis of insulinomas.
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影响因子：
5.2
作者：
Körner M;Christ E;Wild D;Reubi JC
通讯作者：
Reubi JC
DOI：
10.1007/s00259-002-0761-1
发表时间：
2002-05-01
影响因子：
9.1
作者：
Gotthardt, M;Fischer, M;Behr, TM
通讯作者：
Behr, TM
DOI：
10.1038/labinvest.2013.133
发表时间：
2014-01
期刊：
Laboratory investigation; a journal of technical methods and pathology
影响因子：
--
作者：
通讯作者：
--
影响因子：
5.8
作者：
Gough, S. C. L.
通讯作者：
Gough, S. C. L.
DOI：
10.1016/j.bpg.2005.05.008
发表时间：
2005-10-01
影响因子：
3.2
作者：
Grant, CS
通讯作者：
Grant, CS