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.

Peptidomimetic toolbox for drug discovery / Lenci, Elena; Trabocchi, Andrea. - In: CHEMICAL SOCIETY REVIEWS. - ISSN 0306-0012. - STAMPA. - 49(2020), pp. 3262-3277. [10.1039/d0cs00102c]

Peptidomimetic toolbox for drug discovery

Lenci, Elena;Trabocchi, Andrea
2020

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.
49
3262
3277
Goal 3: Good health and well-being
Lenci, Elena; Trabocchi, Andrea
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2158/1189796
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