Site-specific addition of an 18F-N-methylaminooxy-containing prosthetic group to a vinylsulfone modified peptide
✍ Scribed by Dag Erlend Olberg; Ole Kristian Hjelstuen; Magne Solbakken; Joseph M. Arukwe; Knut Dyrstad; Alan Cuthbertson
- Book ID
- 102367500
- Publisher
- John Wiley and Sons
- Year
- 2009
- Tongue
- French
- Weight
- 285 KB
- Volume
- 52
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
Numerous strategies employing prosthetic groups for the radiosynthesis of ^18^F‐fluorinated peptides for positron emission tomography have been investigated in recent years. We have previously reported a novel [^18^F]prosthetic group bearing the N‐methylaminooxy functionality capable of reacting in a site‐selective manner with peptides functionalized with Michael‐acceptors. In a further extension of this methodology we demonstrate that O‐[2‐(2‐[^18^F]fluoroethoxy)ethyl]‐N‐methyl‐N‐hydroxylamine, [^18^F]4, reacts chemoselectively with a vinylsulfone functionalized peptide. The conjugation yields were studied with respect to reaction time, level of radioactivity, peptide concentration and purity of the [^18^F]prosthetic group used in the conjugation reaction. Incubation at 70°C gave conjugation yields of around 80% with high radiochemical purity after 70 min at pH 5 in acetate buffer. Copyright © 2009 John Wiley & Sons, Ltd.