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Structure-Based Virtual Screening Allows the Identification of Efficient Modulators of E-Cadherin-Mediated Cell-Cell
Andrea Dalle Vedove1, Federico Falchi2,3, Stefano Donini1
1Center for Nano Science and Technology @PoliMi, Istituto Italiano di Tecnologia, Via Pascoli 70/3, 20133 Milano, Italy.
International Journal of Molecular Sciences
|August 3, 2019
Summary
Researchers identified novel small molecules that inhibit E-cadherin-mediated cell adhesion. One compound also demonstrated anti-invasive properties, offering potential for cancer drug development.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Cadherins are crucial transmembrane proteins regulating cell adhesion and tissue development.
- Their role in cancer progression and metastasis makes them significant drug targets.
- A druggable interface in cadherins has been identified, enabling modulator design.
Purpose of the Study:
- To identify efficient and selective modulators of E-cadherin-mediated cell-cell adhesion.
- To explore novel therapeutic strategies targeting cadherin interactions in cancer.
Main Methods:
- Structure-based virtual screening was employed to discover potential inhibitors.
- In vitro cell adhesion assays using human pancreatic tumor cells (BxPC-3) were performed.
- Cell invasion assays were conducted to assess anti-invasive properties.
Main Results:
- Two compounds effectively inhibited E-cadherin-mediated cell-cell adhesion at micromolar concentrations.
- One identified compound also exhibited anti-invasive effects in cancer cells.
- These findings validate a strategy for designing cadherin dimerization modulators.
Conclusions:
- Novel selective modulators of E-cadherin adhesion were identified.
- These compounds hold promise for treating cadherin-expressing solid tumors.
- Further development could enhance drug delivery across biological barriers.
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