Rapid one-step <sup>18</sup>F-radiolabeling of biomolecules in aqueous media by organophosphine fluoride acceptors.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 30824691.
- Also identified by DOI 10.1038/s41467-019-08953-0 and PMC identifier 6397219.
- Licence recorded as CC BY.
- The licence permits redistribution, so the abstract is shown in full and the full text is available from the publisher.
Abstract
Currently, only a few <sup>18</sup>F-radiolabeling methods were conducted in aqueous media, with non-macroelement fluoride acceptors and stringent conditions required. Herein, we describe a one-step non-solvent-biased, room-temperature-driven <sup>18</sup>F-radiolabeling methodology based on organophosphine fluoride acceptors. The high water tolerance for this isotope-exchange-based <sup>18</sup>F-labeling method is attributed to the kinetic and thermodynamic preference of F/F over the OH/F substitution based on computational calculations and experimental validation. Compact [<sup>18/19</sup>F]di-tert-butyl-organofluorophosphine and its derivatives used as <sup>18</sup>F-labeling synthons exhibit excellent stability in vivo. The synthons are further conjugated to several biomolecular ligands such as c(RGDyk) and human serum albumin. The one-step labeled biomolecular tracers demonstrate intrinsic target imaging ability and negligible defluorination in vivo. The current method thus offers a facile and efficient <sup>18</sup>F-radiolabeling pathway, enabling further widespread application of <sup>18</sup>F.
Medical subject headings
- Fluorides
- Fluorine Radioisotopes
- Isotope Labeling
- Organofluorophosphonates
- Water