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Updated: Jun 11, 2026
Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Click chemistry for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin
G Ferro-Flores1, I A Rivero, C L Santos-Cuevas
1Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera México-Toluca S/N, La Marquesa, Ocoyoacac, Estado de México, C.P. 52750, México. ferro_flores@yahoo.com.mx
Abstract:
(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.
