Design of RGD-ATWLPPR peptide conjugates for the dual targeting of $\alpha$V$\beta$3 integrin and neuropilin-1.
Targeting the tumor microenvironment is a promising strategy to detect and/or treat cancer. The design of selective compds. that co-target several receptors frequently overexpressed in solid tumors may allow a reliable and selective detection of tumors. Here we report the modular synthesis of compds. encompassing ligands of $\alpha$V$\beta$3 integrin and neuropilin-1 that are overexpressed in the tumor microenvironment. These compds. were then evaluated through cellular expts. and imaging of tumors in mice. We obsd. that the peptide that displays both ligands is more specifically accumulating in the tumors than in controls. Simultaneous interaction with $\alpha$V$\beta$3 integrin and NRP1 induces NRP1 stabilization at the cell membrane surface which is not obsd. with the co-injection of the controls. [on SciFinder(R)]
Références
- Titre
- Design of RGD-ATWLPPR peptide conjugates for the dual targeting of $\alpha$V$\beta$3 integrin and neuropilin-1.
- Type de publication
- Article de revue
- Année de publication
- 2018
- Auteurs
- Thoreau, Fabien, Vanwonterghem Laetitia, Henry Maxime, Coll Jean-Luc, and Boturyn Didier
- Revue
- Org. Biomol. Chem.
- Volume
- 16
- Pagination
- 4101–4107
- ISSN
- 1477-0520
- Mots-clés
- antitumor agent tumor target integrin neuropilin cell membrane pharmacokinetic peptide conjugate design synthesis tumor imaging agent drug target pharmacokinetic fluorescence confocal microscopy RGT peptide conjugate NRP1 oxime ligation azide alkyne cycloaddn solid phase peptide synthesis cyclization
Soumis le 5 avril 2019