Fluorine reactivity with metals11/5/2023 In this process, the positron and electron are converted into a pair of photons with energies of 511 keV which are emitted at ca. These imaging agents, radiolabeled with a radionuclide that decays via β + decay, release a positron (β +) which upon collision with an electron in the surrounding matter results in annihilation. PET is primarily based on radiolabeled small-molecule probes that serve as imaging agents. First used to detect brain tumors prior to surgical removal in the 1950s ( Sweet, 1951 Wrenn et al., 1951), it is now used in the study of cardiac diseases ( Robinson and Bourque, 2019) and myocardial perfusions ( Driessen et al., 2017), neurodegenerative diseases such as Parkinson’s ( Walker et al., 2018), Alzheimer’s ( Chandra et al., 2019) and Huntington’s ( Cybulska et al., 2020) diseases, inflammatory diseases ( Wu et al., 2013), cancers including those that affect the breasts ( Dijkers et al., 2009 Kurihara et al., 2015), lungs ( De Ruysscher et al., 2012), skin ( Duncan et al., 2016) and prostate ( Jadvar, 2013), as well as diseases caused by bacterial infections ( Auletta et al., 2019). Positron emission tomography (PET) is a powerful, minimally invasive molecular imaging technique. The potential for these techniques to be used for the direct, aqueous radiolabeling of proteins with fluoride is discussed. This review explores radiofluorination through bond formation with fluoride at boron, metal complexes, silicon, phosphorus and sulfur. But, when it comes to the radiofluorination of proteins, these indirect methods are not always suited to the short half-life of the fluorine-18 radionuclide (110 min). To circumvent these issues, indirect fluorination methods making use of prosthetic groups that are first fluorinated and then conjugated to a protein have become commonplace. The aqueous environments required by proteins severely hampers fluorination yields while the dry, organic solvents that promote nucleophilic fluorination can denature proteins. The direct fluorination of native proteins through C-F bond formation is, however, a difficult task. The ability to radiolabel proteins with fluoride enables the use of positron emission tomography (PET) for the early detection, staging and diagnosis of disease.
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