Crystal Structure of Human E-Cadherin-EC1EC2 in Complex with a Peptidomimetic Competitive Inhibitor of Cadherin Homophilic Interaction

Valentina Nardone, Anna Paola Lucarelli, Andrea Dalle Vedove, Roberto Fanelli, Antonella Tomassetti, Laura Belvisi, Monica Civera, Emilio Parisini

Research output: Contribution to journalArticlepeer-review

Abstract

Cadherins are transmembrane cell adhesion proteins whose aberrant expression often correlates with cancer development and proliferation. We report the crystal structure of an E-cadherin extracellular fragment in complex with a peptidomimetic compound that was previously shown to partially inhibit cadherin homophilic adhesion. The structure reveals an unexpected binding mode and allows the identification of a druggable cadherin interface, thus paving the way to a future structure-guided design of cell adhesion inhibitors against cadherin-expressing solid tumors.

Original languageEnglish
Pages (from-to)5089-5094
Number of pages6
JournalJournal of Medicinal Chemistry
Volume59
Issue number10
DOIs
Publication statusPublished - May 26 2016

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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