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CAPPELLA — Result In Brief

Project ID: 37251
Country: Switzerland

Targeting protein-protein interactions in cancer

After many years of research, cancer therapy remains a big puzzle for scientists. A European initiative investigated the potential of inhibiting interaction of known cancer-related proteins as a specific anti-cancer treatment.
Targeting protein-protein interactions in cancer
Disrupting the interaction of key proteins within cells constitutes an emerging new field in drug design. However, protein-protein interactions (PPIs) differ structurally from more classical drug targets such as enzymes and receptors, challenging the development of compounds that could effectively target PPIs.

By bringing together Europe's leading biotech companies and highly recognised academic institutions, the EU-funded project 'Combating cancer through novel approaches to protein-protein interaction inhibitor libraries' (CAPPELLA) aimed to develop a series of innovative small-ligand tools and libraries to inhibit PPIs in cancer.

Using in silico, chemical and genetic methods, project partners wished to target three known PPIs namely BRCA2-Rad51, p53-Mdm2 and betacatenin-TCF4. These protein pairs are involved in key signalling pathways implicated in cancer.

Specific readout assays were developed in order to detect disruption of these PPIs. Over 6,000 compounds derived from bio-sources of natural origin or marine extracts were screened and putative candidates were identified.

Computational ‘pharmacophore’ models were built for virtual screening of the three targets and of databases in order to further validate inhibitory compounds that could be produced by medicinal chemistry. Six new compound families were identified for the three targets and were biologically tested for efficiency.

The CAPPELLA project proposed novel solutions for specifically disrupting known cancer PPIs. Identified compounds constitute promising treatment and therapeutic approaches for various types of cancer.

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