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- PMID: 20435481
- UKPMCID: 20435481
- DOI: 10.1016/j.apradiso.2010.04.007
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Radiolabeling with fluorine-18 of a protein, interleukin-1 receptor antagonist.
Prenant, C; Cawthorne, C; Fairclough, M; Rothwell, N; Boutin, H
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine. 2010;68(9):1721-7.
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Full-text held externally
- PMID: 20435481
- UKPMCID: 20435481
- DOI: 10.1016/j.apradiso.2010.04.007
Abstract
IL-1RA is a naturally occurring antagonist of the pro-inflammatory cytokine interleukin-1 (IL-1) with high therapeutic promise, but its pharmacokinetic remains poorly documented. In this report, we describe the radiolabeling of recombinant human interleukin-1 receptor antagonist (rhIL-1RA) with fluorine-18 to allow pharmacokinetic studies by positron emission tomography (PET). rhIL-1RA was labeled randomly by reductive alkylation of free amino groups (the epsilon-amino group of lysine residues or amino-terminal residues) using [(18)F]fluoroacetaldehyde under mild reaction conditions. Radiosyntheses used a remotely controlled experimental rig within 100min and the radiochemical yield was in the range 7.1-24.2% (decay corrected, based on seventeen syntheses). We showed that the produced [(18)F]fluoroethyl-rhIL-1ra retained binding specificity by conducting an assay on rat brain sections, allowing its pharmakokinetic study using PET.