Issue 23, 2011

Inorganic approaches for radiolabelling biomolecules with fluorine-18 for imaging with Positron Emission Tomography

Abstract

Conventional methods for radiolabelling biomolecules such as proteins and peptides with fluorine-18 for PET imaging rely on carbon–fluorine bond formation and are complex and inefficient. Several non-carbon elements form strong bonds (i.e. with high bond enthalpy) with fluorine, but with lower activation energy for their formation compared to carbon–fluorine bonds, whilst preserving a relatively high kinetic stability. In particular, by incorporating boron-, aluminium- and silicon-containing prosthetic groups into biomolecules, promising results have recently been achieved in the radiolabelling with F-18-fluoride under mild aqueous conditions, affording a level of convenience, efficiency and specific activity potentially superior to those offered by conventional C–F bond formation methods. The promise already shown by these early studies heralds a new branch of bioconjugate radiochemistry involving a wider range of “fluoridephilic” elements for synthesis of PET molecular imaging agents.

Graphical abstract: Inorganic approaches for radiolabelling biomolecules with fluorine-18 for imaging with Positron Emission Tomography

Article information

Article type
Perspective
Submitted
16 Nov 2010
Accepted
21 Feb 2011
First published
15 Apr 2011

Dalton Trans., 2011,40, 6196-6205

Inorganic approaches for radiolabelling biomolecules with fluorine-18 for imaging with Positron Emission Tomography

G. E. Smith, H. L. Sladen, S. C. G. Biagini and P. J. Blower, Dalton Trans., 2011, 40, 6196 DOI: 10.1039/C0DT01594F

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