Novel nucleolin-binding peptides and their applications

By developing multiple antigen peptides (AGM series) that specifically bind nucleolin, the stability and targeting of nanoparticles and antibody drug carriers are solved, and the efficient accumulation and anti-cancer effects of chemotherapy drugs in cancer cells are achieved, providing a new method for cancer diagnosis and treatment.

CN115811990BActive Publication Date: 2025-08-29ANIGEN CO LTD
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Patent Information

Application Number
CN202180049591.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Priority Date
2020-05-19
Filing Date
2021-05-18
Publication Date
2025-08-29
Estimated Expiration
2041-05-18

AI Technical Summary

Technical Problem

In the existing cancer treatment, nanoparticles and antibody drug carriers have problems with circulation instability, insufficient tissue distribution and cytotoxicity. Peptide ligands have short half-life due to enzyme cleavage, making it difficult to effectively target the delivery of chemotherapy drugs.

Method used

Using OBOC combination method and MAP synthesis technology, multiple antigen peptides (AGM series) specifically binding to nucleolin were developed and coupled to chemotherapeutic drugs to form peptide conjugates and fusion peptides for specific targeting of cancer cells.

Benefits of technology

It improves the accumulation and cytotoxicity of chemotherapy drugs in cancer cells, enhances the anti-cancer effect, reduces systemic toxicity, and provides new tools for cancer diagnosis and treatment.

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Abstract

The present invention relates to a novel peptide that specifically binds to nucleolin, and more specifically, to a peptide expressed by a specific amino acid sequence, a conjugate comprising the peptide and an anticancer drug, a fusion peptide comprising the peptide and a cell-penetrating peptide, a composition comprising the peptide for diagnosing cancer, and a composition comprising the peptide or the conjugate for preventing or treating cancer. In the present invention, the peptide ligand AGM peptide and its mutants, screened using the MAP synthesis method and the OBOC combination method, have been shown to specifically bind to cancer cells, and their conjugates with anticancer drugs inhibit cancer growth (in vitro and in vivo). Therefore, the AGM peptide targeting nucleolin can be effectively used for diagnosis and targeted drug delivery in cancer treatment.
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