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Issue 11, 2020
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Peptidomimetic toolbox for drug discovery

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Abstract

The art of transforming peptides into drug leads is still a dynamic and fertile field in medicinal chemistry and drug discovery. Peptidomimetics can respond to peptide limitations by displaying higher metabolic stability, good bioavailability and enhanced receptor affinity and selectivity. Various synthetic strategies have been developed over the years in order to modulate the conformational flexibility and the peptide character of peptidomimetic compounds. This tutorial review aims to outline useful tools towards peptidomimetic design, spanning from local modifications, global restrictions and the use of secondary structure mimetics. Selected successful examples of each approach are presented to document the relevance of peptidomimetics in drug discovery.

Graphical abstract: Peptidomimetic toolbox for drug discovery

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Article information


Submitted
07 Feb 2020
First published
07 Apr 2020

Chem. Soc. Rev., 2020,49, 3262-3277
Article type
Tutorial Review

Peptidomimetic toolbox for drug discovery

E. Lenci and A. Trabocchi, Chem. Soc. Rev., 2020, 49, 3262
DOI: 10.1039/D0CS00102C

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