Design, synthesis and evaluation of RGD peptidomimetic – Gold nanostar conjugates as M21 cell adhesion inhibitors

Year: 2022

Authors: Innocenti R.; Dallari C.; Lenci E.; Pavone F.S.; Bianchini F.; Credi C.; Trabocchi A.

Autors Affiliation: Department of Chemistry “”Ugo Schiff””, University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy; European Laboratory for Non-linear Spectroscopy (LENS), University of Florence, Sesto Fiorentino, Florence, Italy; National Institute of Optics -National Research Council (CNR-INO), Sesto Fiorentino, Florence, Italy; Department of Physics, University of Florence, Sesto Fiorentino, Florence, Italy; Department of Experimental and Clinical Biomedical Sciences “”Mario Serio””, University of Florence, Viale Morgagni 50, Florence, 50134, Italy

Abstract: Effective targeting of alpha vS3 integrin is of high relevance in cancer research as this protein is overexpressed on several types of tumor cells, making such receptor ideal for the development of therapeutics and of diagnostic imaging agents. In this paper, the synthesis of a novel functionalized triazole-based RGD peptidomimetic and its covalent conjugation on pegylated gold nanostars is reported. These highly stable nanoconstructs showed a multivalent effect in binding alpha vS3 integrin receptors and proved to inhibit M21 cell adhesion at 25 pM concentration. Thanks to their peculiar surface plasmon resonance in the “”NIR transparent window””, targeted gold nanostars may represent a promising agent for anticancer multi-modality treatments. 2009 Elsevier Ltd. All rights reserved.


Volume: 126      Pages from: 105873-1  to: 105873-9

More Information: MIUR (“Progetto Dipartimenti di Eccellenza 2018-2022”) , Fondazione Cassa di Risparmio di Pistoia e Pescia and Fondo di Beneficenza Intesa Sanpaolo 2019 (B/2019/0289) are acknowledged for financial support. The authors also wish to acknowledge Fulvio Ratto, Sonia Centi and Roberto Pini (Institute of Applied Physics ´N. Carrara´, CNR-Florence, Italy) and the Centre for Electron Microscopies (Ce.ME) .
KeyWords: Integrin; Bioconjugate chemistry; Drug delivery; Targeted therapy; Cancer
DOI: 10.1016/j.bioorg.2022.105873