Bicyclic peptides are positioned in a privileged spot between small compounds and large antibodies. Like small compounds, bicyclic peptides are conformationally constrained and stable molecules. Like large antibodies, different bicycles can bind to different sites of the target protein, delivering exceptional target selectivity. These outstanding properties make them promising next-generation pharmaceuticals. Our group has developed biocompatible chemical strategies to selectively generate mono- and bicyclic peptides from linear precursors which are readily available via solid-phase peptide synthesis. This chemistry allows us to generate cyclic peptides directly during drug screening campaigns. This project will capitalise on these achievements and explore biocompatible synthetic routes to various kinds of bicycles and their applications in drug discovery.

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