title: 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.
authors.affiliation: King's College London, Division of Imaging Sciences, St Thomas' Hospital, 4th Floor Lambeth Wing, London, UK SE1 7EH.
authors.forename: Gareth E
authors.initials: GE
authors.lastname: Smith
authors.forename: Helen L
authors.initials: HL
authors.lastname: Sladen
authors.forename: Stefano C G
authors.initials: SC
authors.lastname: Biagini
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Blower
mesh_terms: D000535:Aluminum / Q000737:chemistry; D000818:Animals; D001895:Boron / Q000737:chemistry; D002614:Chelating Agents / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling; D051379:Mice; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics; D012825:Silicon / Q000737:chemistry; D014018:Tissue Distribution
chemical_list: D002614:Chelating Agents; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D000535:Aluminum; D001895:Boron; D012825:Silicon