Background: Peptides are usually used to investigate regulatory networks and protein function.
They can also be used in therapeutic research: They are employed both to identify and later to
validate therapeutical target and in drug discovery processes. Their development enables the identification
of several protein surfaces as crucial therapeutic targets and to promote the discovery of small
drugs specific for these molecular interfaces.
Methods: This review was developed through the research of online content and patents related to
natural and de novo designed peptides in neurological diseases studies. The effects of natural and derived
peptides and/or peptidomimetic on models of neurodegenerative diseases and other neurological disorders were
Results: Many peptides are frequently identified as receptor antagonists, inhibitors of protein–protein interactions and
several of them and/or peptide-derived compounds are commercial drugs or in clinical trials. Thus, peptide research could
play a crucial role in the identification of protein ligands. Despite these favorable properties, they present low bioavailability
and metabolic stability respect with traditional drugs. New synthetic strategies for limiting metabolic degradation
and alternative routes of administration have been conceived to enlarge the number of peptide-based drugs in preclinical
Conclusion: Peptide-based drug discovery is an important option to address common therapeutic challenges including
human neurological diseases.