Fluorine‐18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [18F]FPyME |
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Authors: | Charlotte L Denholt Bertrand Kuhnast Frédéric Dollé Francoise Hinnen Paul R Hansen Nic Gillings Andreas Kjær |
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Institution: | 1. PET & Cyclotron Unit, Copenhagen University Hospital, Rigshospitalet, 2100 Copenhagen, Denmark;2. CEA, Institut d'imagerie biomédicale, Service hospitalier Frédéric Joliot, 91406 Orsay, France;3. Department of Natural Science, University of Copenhagen, 2100 Copenhagen, Denmark;4. Cluster for Molecular Imaging, University of Copenhagen, 2200 Copenhagen, Denmark |
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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. Copyright © 2010 John Wiley & Sons, Ltd. |
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Keywords: | targeting peptides fluorine‐18 labelling [18F]FPyME EGFRvIII cancer PET |
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