Protein-protein interacti1 Helix mimetics act as PPI inhibitors by matching the spatial topography of an α-helix by presenting binding groups in the same orientation as ‘hot spot’ amino acid residues.2,3
This presentation will describe the ability of a library of helix mimetics to inhibit key protein-protein interactions involved in the development of cancer including characterisation of their intracellular target engagement.2 Future efforts to expand the approach to more complex targets with novel scaffolds will also be discussed
1. V.Azzarito, K. Long, N.S. Murphy, A.J. Wilson, Nature Chem, 2013, 5, 161.
2. A. Barnard et al. Angew. Chem. Int. Ed. 2015, 54, 2690.
3. A. Barnard et al. Org. Biomol. Chem. 2014, 12, 6794.
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