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Bioorg Med Chem Lett. 2013 Nov 15;23(22):6068-72. doi: 10.1016/j.bmcl.2013.09.031. Epub 2013 Sep 19.

Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [18F]FPPA-c(RGDfK).

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Cyclotron Unit, University Hospital of Geneva, Rue Gabrielle Perrte-Gentil 4, Geneva 1211, Switzerland; School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Quai Ernest Ansermet 30, Geneva 1211, Switzerland.


The development of RGD-based antagonist of αvβ3 integrin receptor has enhanced the interest in PET probes to image this receptor for the early detection of cancer, to monitor the disease progression and the response to therapy. In this work, a novel prosthetic group (N-(4-fluorophenyl)pent-4-ynamide or FPPA) for the (18)F-labeling of an αvβ3 selective RGD-peptide was successfully prepared. [(18)F]FPPA was obtained in three steps with a radiochemical yield of 44% (decay corrected). Conjugation to c(RGDfK(N3)) by the Cu(II) catalyzed Huisgen azido alkyne cycloaddition provided the [(18)F]FPPA-c(RGDfK) with a radiochemical yield of 29% (decay corrected), in an overall synthesis time of 140 min.


Click chemistry; Positron emission tomography; [(18)F]-labeling; c(RGDfK); αvβ3 Integrin

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