High-yielding aqueous 18F-labeling of peptides via Al18F chelation |
| |
Authors: | D'Souza Christopher A McBride William J Sharkey Robert M Todaro Louis J Goldenberg David M |
| |
Institution: | Immunomedics Inc., 300 American Road, Morris Plains, New Jersey 07950, USA. cdsouza@immunomedics.com |
| |
Abstract: | The coordination chemistry of a new pentadentate bifunctional chelator (BFC), NODA-MPAA 1, containing the 1,4,7-triazacyclononane-1,4-diacetate (NODA) motif with a methylphenylacetic acid (MPAA) backbone, and its ability to form stable Al(18)F chelates were investigated. The organofluoroaluminates were easily accessible from the reaction of 1 and AlF(3). X-ray diffraction studies revealed aluminum at the center of a slightly distorted octahedron, with fluorine occupying one of the axial positions. The tert-butyl protected prochelator 7, which can be synthesized in one step, is useful for coupling to biomolecules on solid phase or in solution. High yield (55-89%) aqueous (18)F-labeling was achieved in 10-15 min with a tumor-targeting peptide 4 covalently linked to 1. Defluorination was not observed for at least 4 h in human serum at 37 °C. These results demonstrate the facile application of Al(18)F chelation using BFC 1 as a versatile labeling method for radiofluorinating other heat-stable peptides for positron emission imaging. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|