18F-fluorothiols: a new approach to label peptides chemoselectively as potential tracers for positron emission tomography |
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Authors: | Glaser Matthias Karlsen Hege Solbakken Magne Arukwe Joseph Brady Frank Luthra Sajinder K Cuthbertson Alan |
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Institution: | Hammersmith Hospital, Hammersmith Imanet Ltd., Du Cane Road, London W12 0NN, U.K. mglaser@csc.mrc.ac.uk |
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Abstract: | (18)F]Fluorothiols are a new generation of peptide labeling reagents. This article describes the preparation of suitable methanesulfonyl precursors and their use in no-carrier-added radiosyntheses of (18)F-fluorothiols. The preparations of (3-(18)F]fluoropropylsulfanyl)triphenylmethane, (2-2-2-(2-(18)F]fluoroethoxy)ethoxy]ethoxy]ethylsulfanyl)triphenylmethane, and 4-(18)F]fluoromethyl-N-2-triphenylmethanesulfanyl)ethyl]benzamide starting from the corresponding methanesulfonyl precursors were investigated. Following the removal of the triphenylmethane protecting group, the (18)F-fluorothiols were reacted with the N-terminal chloroacetylated model peptide ClCH(2)C(O)-LysGlyPheGlyLys. The corresponding radiochemical yields of (18)F-labeled isolated model peptide, decay-corrected to (18)F fluoride, were 10%, 32%, and 1%, respectively. These results indicate a considerable potential of (18)F-fluorothiols for the chemoselective labeling of peptides as tracers for positron emission tomography (PET). |
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