Long-acting polypeptides for npr-b targeting and uses thereof in bone system disorders

CN119529033BActive Publication Date: 2026-06-19SUN YAT SEN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SUN YAT SEN UNIV
Filing Date
2024-12-02
Publication Date
2026-06-19

AI Technical Summary

Technical Problem

Existing peptide compounds, such as vosolide, have short half-lives in vivo, requiring frequent administration, which increases the economic and psychological burden on patients and is costly, making it difficult to meet clinical needs.

Method used

An ultra-long-acting peptide targeting NPR-B was designed and manually synthesized using the Fmoc/t-Bu strategy. Specific amino acid sequences were linked and side chains were grafted to form disulfide bonds, extending the peptide's half-life in vivo. The preparation method included solid-phase synthesis, deprotection, and purification.

Benefits of technology

It significantly prolongs the half-life of the peptide, reaching more than 300 times that of CNP22, reducing the frequency of medication, alleviating the burden on patients, and exhibiting good biological activity and stability, making it suitable for the treatment of skeletal system diseases.

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Abstract

This invention relates to the field of biomedical technology, specifically to an ultra-long-acting polypeptide for NPR-B targeting and its application in skeletal system diseases. The ultra-long-acting polypeptide has the following amino acid sequence representing its parent peptide: R1-Gly-Leu-Ser-Lys(R2)-Gly-[Cys-Phe-Gly-Leu-Lys-Leu-Asp-Arg-Ile-Gly-Ser-X1-Ser-Gly-Leu-Gly-Cys]-R3 (disulfide ring formation). The prepared ultra-long-acting polypeptide can significantly prolong its half-life in rats, overcoming the limitation of the endogenous NPR-B agonist C-type natriuretic peptide being unsuitable for drug development due to its short half-life. It also exhibits better biological activity, safety, stability, high synthetic yield, and low cost, and can be used to prepare drugs for treating skeletal system diseases.
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