A shuttle peptide targeting YY1 S247 phosphorylation and its application

CN119708158BActive Publication Date: 2026-05-26ZHONGSHAN HOSPITAL FUDAN UNIV

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHONGSHAN HOSPITAL FUDAN UNIV
Filing Date
2024-12-25
Publication Date
2026-05-26

AI Technical Summary

Technical Problem

Existing EGFR-TKI treatments for EGFR-mutant non-small cell lung cancer patients have encountered resistance issues, and immune checkpoint inhibitors have poor efficacy in combination therapy. There is a need to develop new immunotherapy regimens to enhance efficacy and improve patient prognosis.

Method used

A shuttle peptide targeting YY1 S247 phosphorylation was designed to competitively inhibit phosphorylation at the YY1 S247 site, thereby suppressing CD24 expression and enhancing the therapeutic effect of EGFR-TKI.

Benefits of technology

Shuttle peptides can effectively penetrate cell membranes and nuclear membranes, specifically inhibit phosphorylation at the YY1 S247 site, reduce CD24 expression, enhance the therapeutic effect of EGFR-TKIs, improve the efficacy against EGFR-mutant lung adenocarcinoma, and promote the phagocytosis of tumor cells by macrophages.

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Abstract

This invention discloses a shuttle peptide targeting YY1S247 phosphorylation and its application. The sequence of the shuttle peptide is shown in SEQ ID NO: 1. RQIKIWFQNRRMKWKK is a part of the Drosophila melanogaster tentacles peptide, used to provide cell penetration; PKKKRKV is the nuclear localization sequence of the SV40 large T antigen, used to guide the peptide into the cell nucleus; QIIGENSPPDYSE is the surrounding sequence of the YY1S247 site. The results show that the shuttle peptide (CPP) of this invention can competitively and specifically inhibit phosphorylation at the YY1S247 site, thereby inhibiting CD24 expression and enhancing the therapeutic effect of EGFR-TKIs.
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