Fragment-based approach applied to the discovery of protein-protein interactions stabilisers

Dario Valenti, Stanimira Hristeva, Christian Ottmann, Anna Karawajczyk


Protein-protein interactions (PPIs) are constituents of numerous biological pathways and offer therapeutic intervention points into different pathologies such as cancer1, inflammation2, neurodegenerative3 and metabolic diseases4. Particularly, stabilisation of complexes showed to play a key role in biological pathways offering an additional access point to their modulation. Since this approach has not yet been explored in a systematic way, the TASPPI (TArgeted small-molecule Stabilisation of Protein-Protein Interactions) consortium5 aims to identify chemical PPI stabilisers in order to develop new crucial therapeutic strategies in the treatment of the disease areas mentioned above.

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