Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 53, Issue 34, Pages 8913-8918Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201403345
Keywords
bioconjugated peptides; enzyme catalysis; fluorinase; fluorine-18; positron emission tomography
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Funding
- ERC
- EPSRC
- Scottish Imaging Network (SINAPSE)
- John and Kathleen Watson Scholarship
- EPSRC [EP/I034734/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/C000080/1] Funding Source: researchfish
- Engineering and Physical Sciences Research Council [EP/I034734/1] Funding Source: researchfish
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A strategy for last-step F-18 fluorination of bioconjugated peptides is reported that exploits an Achilles heel in the substrate specificity of the fluorinase enzyme. An acetylene functionality at the C-2 position of the adenosine substrate projects from the active site into the solvent. The fluorinase catalyzes a transhalogenation of 5'-chlorodeoxy-2-ethynyladenosine (CID EA) to 5'-fluorodeoxy-2-ethynyladenosine (FDEA). Extending a polyethylene glycol linker from the terminus of the acetylene allows the presentation of bioconjugation cargo to the enzyme for F-18 labelling. The method uses an aqueous solution ((H2O)-O-18) of [F-18]fluoride generated by the cyclotron and has the capacity to isotopically label peptides of choice for positron emission tomography (PET).
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