Click chemistry for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin.
(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.
Ferro-Flores
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G
Departamento 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
Rivero
I A
IA
Santos-Cuevas
C L
CL
Sarmiento
J I
JI
Arteaga de Murphy
C
C
Ocampo-García
B E
BE
García-Becerra
R
R
Ordaz-Rosado
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D
D000818:Animals; D001839:Bombesin / Q000737:chemistry*; D045744:Cell Line, Tumor; D006801:Humans; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry*
D015609:Organotechnetium Compounds; D001839:Bombesin