4.6 Article

Improved synthesis of , an NIR fluorescence RGD probe targeting αvβ3 integrin

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 21, Issue 42, Pages 8584-8592

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d3ob01206a

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Optical imaging is a non-invasive diagnostic imaging technology that utilizes fluorescent molecules emitting light in the near-infrared region to achieve tumor imaging. It has potential clinical applications.
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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