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: Univ Florence, Dept Chem Ugo Schiff, Via Lastruccia 13, I-50019 Florence, Italy; Univ Florence, European Lab Nonlinear Spect LENS, Florence, Italy; Natl Inst Opt, Natl Res Council CNR INO, Florence, Italy; Univ Florence, Dept Phys, Florence, Italy; Univ Florence, Dept Expt & Clin Biomed Sci Mario Serio, Viale Morgagni 50, I-50134 Florence, Italy; Univ Florence, Dept Chem Ugo Schiff, Florence, Italy; Univ Florence, European Lab Nonlinear Spect LENS, Florence, 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.

Journal/Review: BIOORGANIC CHEMISTRY

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

Citations: 4
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