Selective npy5r agonists with high chemical and metabolic stability
By modifying NPY5R agonists through amino acid substitution and lipolysis, the problem of insufficient chemical and metabolic stability of peptides in existing technologies has been solved, achieving high stability and long-lasting therapeutic effects of peptides and reducing treatment costs.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Filing Date
- 2024-12-20
- Publication Date
- 2026-07-14
AI Technical Summary
Existing selective NPY5R agonists have shortcomings in terms of chemical and metabolic stability, resulting in short drug half-lives, the need for cryogenic storage, and frequent dosing, which increases treatment costs and inconvenience.
A series of peptide mimics were designed to improve their chemical and metabolic stability by introducing amino acid substitutions and lipidation at specific positions, including amino acid sequence optimization at the N-terminus and C-terminus, and lipidation at position X4 of the peptide, thereby improving the stability and selectivity of the peptide.
This approach achieves high chemical and metabolic stability of peptides, prolongs drug half-life, reduces storage and dosing frequency, and lowers treatment costs.
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