Improved synthesis of , an NIR fluorescence RGD probe targeting v3 integrin

Rachele Maschio,Federica Buonsanti, Federico Crivellin, Fulvio Ferretti,Luciano Lattuada,Federico Maisano,Laura Orio, Lorena Pizzuto, Raphael Campanella, Anthony Clouet,Camilla Cavallotti,Giovanni B. Giovenzana

ORGANIC & BIOMOLECULAR CHEMISTRY(2023)

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摘要
Optical imaging (OI) is gaining increasing attention in medicine as a non-invasive diagnostic imaging technology and as a useful tool for image-guided surgery. OI exploits the light emitted in the near-infrared region by fluorescent molecules able to penetrate living tissues. Cyanines are an important class of fluorescent molecules and by their conjugation to peptides it is possible to achieve optical imaging of tumours by selective targeting. We report here the improvements obtained in the synthesis of DA364, a small fluorescent probe (1.5 kDa) prepared by conjugation of pentamethine cyanine Cy5.5 to an RGD peptidomimetic, which can target tumour cells overexpressing integrin alpha v beta 3 receptors.
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