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