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ID: ALA3817797

Journal: J Med Chem

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

Authors: Nardone V, Lucarelli AP, Dalle Vedove A, Fanelli R, Tomassetti A, Belvisi L, Civera M, Parisini E.

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.

CiteXplore: 27120112

DOI: 10.1021/acs.jmedchem.5b01487