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Université de Fribourg

Synthesis of a non-peptidic PET tracer designed for α5β1 integrin receptor

Monaco, Alessandra ; Michelin, Olivier ; Prior, John ; Rüegg, Curzio ; Scapozza, Leonardo ; Seimbille, Yann

In: Journal of labelled compounds & radiopharmaceuticals, 2014, vol. 57, no. 5, p. 365-370

Arginine–glycine–aspartic acid (RGD)-containing peptides have been traditionally used as PET probes to noninvasively image angiogenesis, but recently, small selective molecules for α₅β₁ integrin receptor have been developed with promising results. Sixty-one antagonists were screened, and tert-butyl...

Université de Fribourg

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

Monaco, Alessandra ; Zoete, Vincent ; Alghisi, Gian Carlo ; Rüegg, Curzio ; Michelin, Olivier ; Prior, John ; Scapozza, Leonardo ; Seimbille, Yann

In: Bioorganic & Medicinal Chemistry Letters, 2013, vol. 23, no. 22, p. 6068–6072

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 18F-labeling of an αvβ3 selective RGD-peptide was successfully prepared....