Issue 9, 2015
From the journal:

Organic & Biomolecular Chemistry

Computational design of novel peptidomimetic inhibitors of cadherin homophilic interactions†

Fabio Doro,a   Cinzia Colombo,a   Chiara Alberti,b   Daniela Arosio,c   Laura Belvisi,ac   Cesare Casagrande,a   Roberto Fanelli,d   Leonardo Manzoni,c   Emilio Parisini,e   Umberto Piarulli,d   Elena Luison,b   Mariangela Figini,b   Antonella Tomassetti*b  and  Monica Civera*a  

* Corresponding authors

a Dipartimento di Chimica, Università degli Studi di Milano, Via C. Golgi 19, Milan, Italy
E-mail: monica.civera@unimi.it
Fax: +39 02 50314072
Tel: +39 02 50314061

b Dipartimento di Oncologia Sperimentale e Medicina Molecolare, Fondazione IRCCS Istituto Nazionale dei Tumori, Via G. Amadeo 42, Milan, Italy
E-mail: Antonella.Tomassetti@istitutotumori.mi.it

c CNR – Istituto di Scienze e Tecnologie Molecolari (ISTM), Via C. Golgi 19, I-20133, Milan, Italy

d Dipartimento di Scienza e Alta Tecnologia, Università degli Studi dell'Insubria, Via Valleggio 11, Como, Italy

e Center for Nano Science and Technology @PoliMi, Istituto Italiano di Tecnologia, Via G. Pascoli 70/3, Milan, Italy

Abstract

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.

Graphical abstract: Computational design of novel peptidomimetic inhibitors of cadherin homophilic interactions

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Article information

DOI
https://doi.org/10.1039/C4OB02538E
Article type
Communication
Submitted
04 Dec 2014
Accepted
13 Jan 2015
First published
14 Jan 2015
This article is Open Access
Creative Commons BY-NC license

Org. Biomol. Chem., 2015,13, 2570-2573

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Computational design of novel peptidomimetic inhibitors of cadherin homophilic interactions

F. Doro, C. Colombo, C. Alberti, D. Arosio, L. Belvisi, C. Casagrande, R. Fanelli, L. Manzoni, E. Parisini, U. Piarulli, E. Luison, M. Figini, A. Tomassetti and M. Civera, Org. Biomol. Chem., 2015, 13, 2570 DOI: 10.1039/C4OB02538E

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