Protein-protein interactions (PPIs) regulate virtually all cellular signalling processes thus developing methods to modulate PPIs represents a significant challenge of immense biochemical and medical importance.1 However, methods to target intracellular (PPIs) using synthetic molecules are not well established.2 This presentation will discuss the development of enabling methods to characterise PPIs3 and design inhibitors, focussing on α-helix4 and β-strand5 mediated interactions. A suite of approaches will be described that rely on use of experimentally validated computational predication of hot-spot residues;3 these are used as a template to design inhibitors for instance based on the grafting of key residues onto the solvent exposed faces of coiled-coils.4 Alongside these efforts the use of dynamic ligation screening6 to replace segments of interfacial peptides, piece by piece will be described.

Development of protein-protein interaction inhibitors

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.