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Fluorine‐18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [ 18 F]FPyME
Author(s) -
Denholt Charlotte L.,
Kuhnast Bertrand,
Dollé Frédéric,
Hinnen Francoise,
Hansen Paul R.,
Gillings Nic,
Kjær Andreas
Publication year - 2010
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1795
Subject(s) - labelling , chemistry , peptide , yield (engineering) , epidermal growth factor receptor , combinatorial chemistry , stereochemistry , radiochemistry , receptor , biochemistry , materials science , metallurgy
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.