Comparison study of [18F]FAl-NOTA-PRGD2, [18F]FPPRGD2, and [68Ga]Ga-NOTA-PRGD2 for PET imaging of U87MG tumors in mice.
Comparison study of [18F]FAl-NOTA-PRGD2, [18F]FPPRGD2, and [68Ga]Ga-NOTA-PRGD2 for PET imaging of U87MG tumors in mice.
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DOI：
10.1021/bc200197h
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发表时间：
2011-12-21
影响因子：
4.7
通讯作者：
Chen, Xiaoyuan
中科院分区：
文献类型：
--
作者：
Lang, Lixin;Li, Weihua;Guo, Ning;Ma, Ying;Zhu, Lei;Kiesewetter, Dale O.;Shen, Baozhong;Niu, Gang;Chen, Xiaoyuan
[18F]FpPRGD2是一种F-18标记的二聚体环状RGDyK多肽，通过靶向αvβ3整合素受体，具有良好的血管生成正电子发射计算机断层成像性能。这种放射性示踪剂已被FDA批准用于临床试验。然而，制备该示踪剂所需的耗时的多步骤合成过程可能会阻碍该示踪剂的广泛使用。最近发展的一种使用F-18氟铝络合物标记放射性多肽的方法为简化标记过程提供了一种策略。另一方面，易于制备的[68Ga]标记的NOTA-RGD衍生物也被报道具有用于成像αvβ3整合素受体的良好性能。本研究的目的是制备[18F]FPPRDG2、[18F]FAL-NOTA-PRGD2和[68Ga]Ga-NOTA-PRGD2，并用小动物PET比较它们的药代动力学和肿瘤显像特性。所有这三种化合物在U87 MG肿瘤中都表现出快速和高示踪剂摄取，具有高目标背景比。三种示踪剂在肝脏、肾脏和肌肉中的摄取情况相似，均以肾脏清除为主。总之，[18F]Fal-NOTA-PRGD2和[68Ga]Ga-NOTA-PRGD2具有与[18F]FPPRGD2相似的成像特性和药代动力学。考虑到它们易于制备和良好的成像质量，[18F]FAL-NOTA-PRGD2和[68Ga]NOTA-PRGD2有望替代[18F]FPPRGD2用于肿瘤αvβ3整合素的正电子发射计算机断层显像。
[18F]FPPRGD2, an F-18 labeled dimeric cyclic RGDyK peptide, has favorable properties for PET imaging of angiogenesis by targeting the αvβ3 integrin receptor. This radiotracer has been approved by the FDA for use in clinical trials. However, the time-consuming multiple-step synthetic procedure required for its preparation may hinder the widespread usage of this tracer. The recent development of a method using an F-18 fluoride-aluminum complex to radiolabel peptides provides a strategy for simplifying the labeling procedure. On the other hand, the easy-to-prepare [68Ga]-labeled NOTA-RGD derivatives have also been reported to have promising properties for imaging αvβ3 integrin receptors. The purpose of this study was to prepare [18F]FPPRDG2, [18F]FAl-NOTA-PRGD2, and [68Ga]Ga-NOTA-PRGD2 and to compare their pharmacokinetics and tumor imaging properties using small animal PET. All three compounds showed rapid and high tracer uptake in U87MG tumors with high target-to-background ratios. The uptake in the liver, kidneys and muscle were similar for all three tracers and they all showed predominant renal clearance. In conclusion, [18F]FAl-NOTA-PRGD2 and [68Ga]Ga-NOTA-PRGD2 have imaging properties and pharmacokinetics comparable to those of [18F]FPPRGD2. Considering their ease of preparation and good imaging qualities, [18F]FAl-NOTA-PRGD2 and [68Ga]NOTA-PRGD2 are promising alternatives to [18F]FPPRGD2 for PET imaging of tumor αvβ3 integrin expression.
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影响因子：
4.7
作者：
Thonon, David;Kech, Cecile;Luxen, Andre
通讯作者：
Luxen, Andre
影响因子：
3.1
作者：
Chen, XY;Liu, S;Conti, PS
通讯作者：
Conti, PS
DOI：
10.2967/jnumed.109.066902
发表时间：
2010-03
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
Laverman P;McBride WJ;Sharkey RM;Eek A;Joosten L;Oyen WJ;Goldenberg DM;Boerman OC
通讯作者：
Boerman OC
影响因子：
12.4
作者：
Zhou Y;Chakraborty S;Liu S
通讯作者：
Liu S
影响因子：
4.9
作者：
Yang M;Gao H;Sun X;Yan Y;Quan Q;Zhang W;Mohamedali KA;Rosenblum MG;Niu G;Chen X
通讯作者：
Chen X