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dc.contributor.authorPrenant, C
dc.contributor.authorCawthorne, Christopher
dc.contributor.authorFairclough, M
dc.contributor.authorRothwell, N
dc.contributor.authorBoutin, H
dc.date.accessioned2010-09-14T09:06:57Z
dc.date.available2010-09-14T09:06:57Z
dc.date.issued2010-09
dc.identifier.citationRadiolabeling with fluorine-18 of a protein, interleukin-1 receptor antagonist. 2010, 68 (9):1721-7 Appl Radiat Isoten
dc.identifier.issn0969-8043
dc.identifier.pmid20435481
dc.identifier.doi10.1016/j.apradiso.2010.04.007
dc.identifier.urihttp://hdl.handle.net/10541/111114
dc.description.abstractIL-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.
dc.language.isoenen
dc.subjectRadiolabelingen
dc.titleRadiolabeling with fluorine-18 of a protein, interleukin-1 receptor antagonist.en
dc.typeArticleen
dc.identifier.eissn1872-9800
dc.contributor.departmentWolfson Molecular Imaging Centre, University of Manchester, Manchester, UK. cprenant@cyclopharma.fren
dc.identifier.journalApplied Radiation and Isotopesen
html.description.abstractIL-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.


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