Two Novel PET Radiopharmaceuticals for Endothelial Vascular Cell Adhesion Molecule-1 (VCAM-1) Targeting
| Autor: | Cecilia Marini, Vanessa Cossu, Giorgia Ailuno, Sara Baldassari, Tullio Florio, Silvana Alfei, Gabriele Caviglioli, Sara Pastorino, Gianmario Sambuceti, Guendalina Zuccari, Giuliana Drava, Andrea Petretto |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Pharmaceutical Science
pretargeting 02 engineering and technology 01 natural sciences Umbilical vein Article chemistry.chemical_compound Pharmacy and materia medica DOTA VCAM-1 Cell adhesion Gallium-68 PET avidin-biotin complex imaging inflammation peptide radiopharmaceuticals avidin–biotin complex Pretargeting 010405 organic chemistry Cell adhesion molecule 021001 nanoscience & nanotechnology In vitro 0104 chemical sciences RS1-441 chemistry Biotinylation Cancer research 0210 nano-technology |
| Zdroj: | Pharmaceutics Volume 13 Issue 7 Pharmaceutics 13 (2021): 1025. doi:10.3390/pharmaceutics13071025 info:cnr-pdr/source/autori:Pastorino S.; Baldassari S.; Ailuno G.; Zuccari G.; Drava G.; Petretto A.; Cossu V.; Marini C.; Alfei S.; Florio T.; Sambuceti G.; Caviglioli G./titolo:Two Novel PET Radiopharmaceuticals for Endothelial Vascular Cell Adhesion Molecule-1 (VCAM-1) Targeting/doi:10.3390%2Fpharmaceutics13071025/rivista:Pharmaceutics/anno:2021/pagina_da:1025/pagina_a:/intervallo_pagine:1025/volume:13 Pharmaceutics, Vol 13, Iss 1025, p 1025 (2021) |
| ISSN: | 1999-4923 |
| DOI: | 10.3390/pharmaceutics13071025 |
| Popis: | Atherosclerosis is a chronic progressive disease involving inflammatory events, such as the overexpression of adhesion molecules including the endothelial Vascular Cell Adhesion Molecule-1 (VCAM-1). VCAM-1 is rapidly overexpressed in the first stages of atherosclerosis, thus representing a promising target for early atheroma detection. Two novel Positron Emission Tomography (PET) radiopharmaceuticals (MacroP and NAMP), based on the VCAM-1-binding peptide having sequence VHPKQHRGGSKGC, were synthesized and characterized. MacroP is derived from the direct conjugation of a DOTA derivative with the peptide, while NAMP is a biotin derivative conceived to be employed in a three-step pretargeting system, involving the use of a double-chelating derivative of DOTA. The identity of the newly synthesized radiopharmaceuticals was confirmed by mass spectrometry and, after radiolabeling with 68Ga, both showed high radiochemical purity in vitro tests on human umbilical vein endothelial cells evidenced their VCAM-1 binding ability, with higher radioactive uptake in the case of NAMP. Moreover, NAMP might also be employed in a theranostic approach in association with functionalized biotinylated nanoparticles. |
| Databáze: | OpenAIRE |
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