A resurgence in peptide drug discovery has been realized with the design of novel macrocyclic peptides of varying classes of scaffolds demonstrating promise for tackling intracellular target space. This presentation will highlight recent work exemplifying such macrocyclic peptides developed as proteomimetics of cognate protein-protein interactions, super-diversity peptide libraries, and hybridization with cell-penetrating peptide motifs. Importantly, a significant expansion of ‘classic’ peptide chemical space engaging innovative design technologies that leverage structural biology, computational chemistry and molecular biophysics is being achieved.

Peptide drug hunter: Exploring macrocycle chemical space and design

251st National Meeting (2016)

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