Inorganic approaches for radiolabelling biomolecules with fluorine-18 for imaging with positron emission tomography

Dalton Trans. 2011 Jun 21;40(23):6196-205. doi: 10.1039/c0dt01594f. Epub 2011 Apr 15.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aluminum / chemistry
  • Animals
  • Boron / chemistry
  • Chelating Agents / chemistry
  • Fluorine Radioisotopes / chemistry*
  • Isotope Labeling
  • Mice
  • Positron-Emission Tomography*
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / pharmacokinetics
  • Silicon / chemistry
  • Tissue Distribution

Substances

  • Chelating Agents
  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Aluminum
  • Boron
  • Silicon