Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to αvβ3 integrin with diverse potency, and selected (125)I-labeled compounds proved to interact in vitro and in vivo with αvβ3 integrin expressed by melanoma cells. Two (125)I-compounds containing either 2-aminobenzimidazole or 2-aminopyridine groups as the arginine bioisostere with the capacity to selectively bind cells of highly expressing αvβ3 melanoma xenografts were found using micro-SPECT imaging studies.

Radiosynthesis and micro-SPECT analysis of triazole-based RGD integrin ligands as non-peptide molecular imaging probes for angiogenesis / Bianchini, Francesca; Fabbrizzi, Pierangelo; Menchi, Gloria; Raspanti, Silvia; Bottoncetti, Anna; Passeri, Alessandro; Andreucci, Elena; Guarna, Antonio; Calorini, Lido; Pupi, Alberto; Trabocchi, Andrea. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 23:(2015), pp. 1112-1122. [10.1016/j.bmc.2014.12.065]

Radiosynthesis and micro-SPECT analysis of triazole-based RGD integrin ligands as non-peptide molecular imaging probes for angiogenesis

BIANCHINI, FRANCESCA;FABBRIZZI, PIERANGELO;MENCHI, GLORIA;RASPANTI, SILVIA;BOTTONCETTI, ANNA;PASSERI, ALESSANDRO;ANDREUCCI, ELENA;GUARNA, ANTONIO;CALORINI, LIDO;PUPI, ALBERTO;TRABOCCHI, ANDREA
2015

Abstract

Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to αvβ3 integrin with diverse potency, and selected (125)I-labeled compounds proved to interact in vitro and in vivo with αvβ3 integrin expressed by melanoma cells. Two (125)I-compounds containing either 2-aminobenzimidazole or 2-aminopyridine groups as the arginine bioisostere with the capacity to selectively bind cells of highly expressing αvβ3 melanoma xenografts were found using micro-SPECT imaging studies.
2015
23
1112
1122
Bianchini, Francesca; Fabbrizzi, Pierangelo; Menchi, Gloria; Raspanti, Silvia; Bottoncetti, Anna; Passeri, Alessandro; Andreucci, Elena; Guarna, Antonio; Calorini, Lido; Pupi, Alberto; Trabocchi, Andrea
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1001538
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