Ferro-Flores G, Rivero I A, Santos-Cuevas C L, Sarmiento J I, Arteaga de Murphy C, Ocampo-García B E, García-Becerra R, Ordaz-Rosado D
Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera México-Toluca S/N, La Marquesa, Ocoyoacac, Estado de México, C.P. 52750, México.
Appl Radiat Isot. 2010 Dec;68(12):2274-8. doi: 10.1016/j.apradiso.2010.06.014. Epub 2010 Jun 17.
(99m)Tc-HYNIC labeled Lys(3)-bombesin has shown specific binding to gastrin-releasing peptide receptors (GRP-r) over-expressed in cancer cells. Click chemistry offers an innovative functionalization strategy for biomolecules such as bombesin. The aim of this research was to apply a click chemistry approach for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin and to compare the in vitro MCF7 breast cancer cell uptake and biodistribution profile in mice with that of (99m)Tc-EDDA/HYNIC-Lys(3)-bombesin. The results suggest a higher lipophilicity for (99m)Tc(CO)(3)-triazole-Lys(3)-bombesin which explains its higher in vivo hepatobiliary elimination. Pancreas-to-blood ratio for (99m)Tc(CO)(3)-triazole-Lys(3)-bombesin was 4.46 at 3 h and both bombesin radiopharmaceuticals showed specific recognition for GRP receptors in MCF7 cancer cells. Click chemistry is a reliable approach for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin.
（99m）Tc-HYNIC标记的赖氨酸（3）-蛙皮素已显示出与癌细胞中过表达的胃泌素释放肽受体（GRP-r）特异性结合。点击化学为诸如蛙皮素的生物分子提供了一种创新的功能化策略。本研究的目的是应用点击化学方法对赖氨酸（3）-蛙皮素进行[（99m）Tc（CO）3]标记，并将其在体外MCF7乳腺癌细胞中的摄取和在小鼠体内的生物分布情况与（99m）Tc-EDDA/HYNIC-赖氨酸（3）-蛙皮素进行比较。结果表明，（99m）Tc（CO）3-三唑-赖氨酸（3）-蛙皮素具有更高的亲脂性，这解释了其在体内更高的肝胆清除率。（99m）Tc（CO）3-三唑-赖氨酸（3）-蛙皮素在3小时时的胰腺与血液比值为4.46，两种蛙皮素放射性药物均显示出对MCF7癌细胞中GRP受体的特异性识别。点击化学是对赖氨酸（3）-蛙皮素进行[（99m）Tc（CO）3]标记的可靠方法。
