Design and synthesis of oxytocin glycosides for the treatment of pain and substance use disorder.
Methods Enzymol
; 698: 343-359, 2024.
Article
en En
| MEDLINE
| ID: mdl-38886038
ABSTRACT
Peptide drugs are a promising alternative to classical small molecule therapeutics with diverse applications, ranging from antibiotic resistant infection to prostate cancer. Oxytocin (OT) is a highly evolutionarily conserved peptide neurohormone and has been of interest for pharmaceutical use since 1909. Despite their increased safety profile relative to most small molecule drugs, peptides are poor candidates based on the pharmacokinetic (PK) properties from their peptide nature. Broad application of OT as a drug has been limited by these same PK issues. Several strategies have been proposed to overcome these limitations, among them glycosylation, which was used in combination with other sequence modifications to produce robust antinociception in mouse models, increased selectivity and potency at the OT receptor, and improved stability in rats.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Dolor
/
Oxitocina
/
Diseño de Fármacos
/
Glicósidos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Methods Enzymol
Año:
2024
Tipo del documento:
Article
País de afiliación:
Estados Unidos