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Constrained peptides' time to shine?

Nature Reviews Drug Discovery volume 17, pages 531–533 (2018)Cite this article

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Constrained peptides have long tantalized drug developers with their potential ability to combine the best attributes of antibodies and small molecules. Finally, a handful of constrained peptides are in late-stage clinical trials.

Peptides occupy a kind of Goldilocks space between small chemicals and large biologics, an intriguing area that theoretically combines the best characteristics of each traditional modality into 'just right' therapeutics. Whereas linear peptides tend to twist and flop in ways that make them too flaccid to make good drugs, drug developers have been working away on de novo cyclic peptides to harness increased stability and improved physicochemical characteristics for therapeutic effect. After decades of experimentation with novel constrained peptide formats, a few are at last entering the drug development end game.

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Figure 1: Selected constrained peptide formats.
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  1. Chris Morrison
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Morrison, C. Constrained peptides' time to shine?. Nat Rev Drug Discov 17, 531–533 (2018). https://doi.org/10.1038/nrd.2018.125

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