Apelin receptor agonists and uses thereof
By designing ipalinide or ipalabelatide analogues with increased half-life and improved signal transduction properties, the problems of short half-life and easy desensitization of ipalinide receptor agonists in clinical applications have been solved, achieving effective activation of the ipalinide receptor pathway and improving the therapeutic effect.
Patent Information
- Application Number
- CN202610456165.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-09-25
- Filing Date
- 2024-04-11
- Publication Date
- 2026-06-05
AI Technical Summary
Apalin peptide receptor agonists have issues with short half-life and easy desensitization in clinical studies, which limits their application in treating diseases such as pulmonary hypertension, systemic sclerosis, heart failure with preserved ejection fraction, age-related sarcopenia, and acute kidney injury.
Novel ipparin peptide or ipabera peptide analogues with increased half-life, reduced desensitization, improved signal transduction properties and enhanced stability have been developed. These analogues are modified ipparin peptide receptor agonists by amino acid substitution at specific positions or by partial fusion with a carrier.
This study achieved effective activation of the apalin peptide receptor pathway, reduced internalization and transcriptional downregulation, and improved the efficacy of treating these diseases.