Backbone N-methylation of peptides: Advances in synthesis and applications in pharmaceutical drug development.
Bioorg Chem
; 141: 106892, 2023 12.
Article
en En
| MEDLINE
| ID: mdl-37776681
ABSTRACT
Peptide-based drugs have garnered considerable attention in recent years owing to their increasingly crucial role in the treatment of diverse diseases. However, the limited pharmacokinetic properties of peptides have hindered their full potential. One prominent strategy for enhancing the druggability of peptides is N-methylation, which involves the addition of a methyl group to the nitrogen atom of the peptide backbone. This modification significantly improves the stability, bioavailability, receptor binding affinity and selectivity of peptide drug candidates. In this review, we provide a comprehensive overview of the advancements in synthetic methods for N-methylated peptide synthesis, as well as the associated limitations. Moreover, we explore the versatile effects of N-methylation on various aspects of peptide properties. Furthermore, we emphasize the efforts dedicated to N-methylated peptide pharmaceuticals that have successfully obtained marketing approval.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Péptidos
/
Desarrollo de Medicamentos
Idioma:
En
Revista:
Bioorg Chem
Año:
2023
Tipo del documento:
Article
País de afiliación:
China