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, F., Fabbrizzi, P., Menchi, G., Raspanti, S., Bottoncetti, A., Passeri, A., Andreucci, E., Guarna, A., Calorini, L., Pupi, A., Trabocchi, A.. - 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.
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