Journal
BIOCONJUGATE CHEMISTRY
Volume 22, Issue 9, Pages 1793-1803Publisher
AMER CHEMICAL SOC
DOI: 10.1021/bc200175c
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Funding
- NIH [5R44RR028018]
- National Center for Research Resources, NIH [RR-03037]
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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 (AlF)-F-18 chelates were investigated. The organofluoroaluminates were easily accessible from the reaction of 1 and AlF3. 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 F-18-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 degrees C. These results demonstrate the facile application of (AlF)-F-18 chelation using BFC 1 as a versatile labeling method for radiofluorinating other heat-stable peptides for positron emission imaging.
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