Crystal Structure of Human E-Cadherin-EC1EC2 in Complex with a Peptidomimetic Competitive Inhibitor of Cadherin Homophilic Interaction
详细信息 查看全文
- 作者：Valentina Nardone ; Anna Paola Lucarelli ; Andrea Dalle Vedove ; Roberto Fanelli ; Antonella Tomassetti ; Laura Belvisi ; Monica Civera ; Emilio Parisini
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：May 26, 2016
- 年：2016
- 卷：59
- 期：10
- 页码：5089-5094
- 全文大小：384K
- 年卷期：0
- ISSN：1520-4804
文摘
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.