Computational design of novel peptidomimetic inhibitors of cadherin homophilic interactionsElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ob02538e

Computational design of novel peptidomimetic inhibitors of cadherin homophilic interactionsElectronic supplementary information (ESI) available. See DOI: 10.1039/c4ob02538e

We report a first set of peptidomimetic ligands mimicking the adhesive interface identified by recent crystallographic structures of E- and N-cadherin. Compounds 2 and 3 inhibit adhesion of epithelial ovarian cancer (EOC) cells with improved efficacy compared to the ADH-1 peptide, a N-cadherin antag...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: Doro, Fabio, Colombo, Cinzia, Alberti, Chiara, Arosio, Daniela, Belvisi, Laura, Casagrande, Cesare, Fanelli, Roberto, Manzoni, Leonardo, Parisini, Emilio, Piarulli, Umberto, Luison, Elena, Figini, Mariangela, Tomassetti, Antonella, Civera, Monica
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:We report a first set of peptidomimetic ligands mimicking the adhesive interface identified by recent crystallographic structures of E- and N-cadherin. Compounds 2 and 3 inhibit adhesion of epithelial ovarian cancer (EOC) cells with improved efficacy compared to the ADH-1 peptide, a N-cadherin antagonist that is in early clinical trials in EOC patients. Peptidomimetic 3 mimicking the DWVI adhesive sequence of the cadherin EC1 domain inhibits cadherin-mediated adhesion in epithelial ovarian cancer cells.
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob02538e