Site-specific 18F-labeling of the protein hormone leptin using a general two-step ligation procedure

Robert R. Flavell, Paresh Kothari, Maya Bar-Dagan, Michael Synan, Shankar Vallabhajosula, Jeffrey M. Friedman, Tom W. Muir, Giovanni Ceccarini

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64 Scopus citations


The protein hormone leptin acts to regulate body fat and energy expenditure. Resistance to this hormone is implicated in human obesity and its pathophysiological consequences. In order to gain insight into the mechanism of leptin resistance, an 18F-labeled derivative was developed to study the biodistribution of the hormone using positron emission tomography (PET). A two-step, site specific ligation approach was developed for this purpose, in which an aminooxy-reactive group was incorporated at the C-terminus of leptin using expressed protein ligation (EPL), which was subsequently derivatized with [18F]fluorobenzaldehyde using an aniline-accelerated radiochemical oximation reaction. The modified hormone was shown to be biologically active in vitro and in vivo, and it was applied to PET imaging in ob/ob mice. These protocols will allow for the routine production of site-specifically 18F radiolabeled leptin, as well as other proteins, for use in PET imaging in systems from mouse to man.

Original languageEnglish (US)
Pages (from-to)9106-9112
Number of pages7
JournalJournal of the American Chemical Society
Issue number28
StatePublished - Jul 16 2008
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • General Chemistry
  • Biochemistry
  • Catalysis
  • Colloid and Surface Chemistry


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