用于体内神经降压素受体表达成像的（68）镓标记类肽-肽杂合物的合成。
Synthesis of a (68)ga-labeled peptoid-Peptide hybrid for imaging of neurotensin receptor expression in vivo.
作者信息
Maschauer Simone, Einsiedel Jürgen, Hocke Carsten, Hübner Harald, Kuwert Torsten, Gmeiner Peter, Prante Olaf
机构信息
Laboratory of Molecular Imaging, Clinic of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, D-91054 Erlangen, Germany.
Department of Chemisty and Pharmacy, Emil Fischer Center.
出版信息
ACS Med Chem Lett. 2010 May 21;1(5):224-8. doi: 10.1021/ml1000728. eCollection 2010 Aug 12.
Abstract
The neurotensin receptor subtype 1 (NTS1) represents an attractive molecular target for imaging various tumors. Positron emission tomography (PET) gained widespread importance due to its sensitivity. We combined the design of a metabolically stable neurotensin analogue with a (68)Ga-radiolabeling approach. The (68)Ga-labeled peptoid-peptide hybrid [(68)Ga]3 revealed high stability, specific tumor uptake (0.7%ID/g, 65 min p.i.), and advantageous biokinetics in vivo using HT29 tumor-bearing nude mice. Because of the ability to internalize into NTS1-expressing tumor cells, [(68)Ga]3 proved to be highly suitable for a reliable and practical visualization of NTS1-expressing tumors in vivo by small animal PET.
摘要
神经降压素受体1型（NTS1）是用于多种肿瘤成像的一个有吸引力的分子靶点。正电子发射断层扫描（PET）因其灵敏度而具有广泛的重要性。我们将代谢稳定的神经降压素类似物设计与（68）Ga放射性标记方法相结合。（68）Ga标记的类肽-肽杂合物[（68）Ga]3显示出高稳定性、特异性肿瘤摄取（注射后65分钟时为0.7%ID/g），并且在荷HT29肿瘤的裸鼠体内具有有利的生物动力学。由于能够内化进入表达NTS1的肿瘤细胞，[（68）Ga]3被证明非常适合通过小动物PET在体内对表达NTS1的肿瘤进行可靠且实用的可视化。
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