Fluorine-18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [18F]FPyME

Charlotte L. Denholt; Bernard Kuhnast; Frédéric Dollé; Francoise Hinnen; Paul Robert Hansen; Nic Gillings; Andreas Kjær

doi:10.1002/jlcr.1795

Fluorine-18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [¹⁸F]FPyME

Charlotte L. Denholt, Bernard Kuhnast, Frédéric Dollé, Francoise Hinnen, Paul Robert Hansen, Nic Gillings, Andreas Kjær

6 Citations (Scopus)

Abstract

There is growing interest in the use of radiolabelled peptides as receptor targeting agents for diagnostic imaging of various cancer types using positron emission tomography. In this work, 1-[3-(2-[¹⁸F]fluoropyridin-3- yloxy)propyl]pyrrole-2,5-dione ([¹⁸F]FPyME) has been used for parallel fluorine-18 labelling of PEPHC1, a peptide selective towards the cancer-specific mutation of the epidermal growth factor receptor (EGFRvIII), and a number of truncated and mutated analogues. Conjugation of the peptides with [¹⁸F]FPyME was achieved within 10 min in non-decay-corrected radiochemical yields of 30-50%. The high yield of the conjugation reaction combined with its short synthesis time allows the labelling of several peptides from a single batch of [¹⁸F]FPyME.

Original language	English
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	53
Issue number	13
Pages (from-to)	774-778
Number of pages	5
ISSN	0362-4803
DOIs	https://doi.org/10.1002/jlcr.1795
Publication status	Published - Nov 2010

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Fluorine-18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [¹⁸F]FPyME. / Denholt, Charlotte L.; Kuhnast, Bernard; Dollé, Frédéric et al.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 53, No. 13, 11.2010, p. 774-778.

Research output: Contribution to journal › Journal article › Research › peer-review

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abstract = "There is growing interest in the use of radiolabelled peptides as receptor targeting agents for diagnostic imaging of various cancer types using positron emission tomography. In this work, 1-[3-(2-[18F]fluoropyridin-3- yloxy)propyl]pyrrole-2,5-dione ([18F]FPyME) has been used for parallel fluorine-18 labelling of PEPHC1, a peptide selective towards the cancer-specific mutation of the epidermal growth factor receptor (EGFRvIII), and a number of truncated and mutated analogues. Conjugation of the peptides with [18F]FPyME was achieved within 10 min in non-decay-corrected radiochemical yields of 30-50%. The high yield of the conjugation reaction combined with its short synthesis time allows the labelling of several peptides from a single batch of [18F]FPyME.",

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AU - Hinnen, Francoise

AU - Hansen, Paul Robert

AU - Gillings, Nic

AU - Kjær, Andreas

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