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

✍ Scribed by Charlotte L. Denholt; Bertrand Kuhnast; Frédéric Dollé; Francoise Hinnen; Paul R. Hansen; Nic Gillings; Andreas Kjær

• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: French
• Weight: 153 KB
• Volume: 53
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1795

✦ Synopsis

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‐[^18^F]fluoropyridin‐3‐yloxy)propyl]pyrrole‐2,5‐dione ([^18^F]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 [^18^F]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 [^18^F]FPyME. Copyright © 2010 John Wiley & Sons, Ltd.