Jump to main content
Jump to site search

Issue 11, 2020
Previous Article Next Article

Peptidomimetic toolbox for drug discovery

Author affiliations


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

Back to tab navigation

Article information

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

Social activity

Search articles by author