Issue 11, 2020

Peptidomimetic toolbox for drug discovery

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

Article information

Article type
Tutorial Review
Submitted
07 2 2020
First published
07 4 2020

Chem. Soc. Rev., 2020,49, 3262-3277

Peptidomimetic toolbox for drug discovery

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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements