SR-B1 targeted polypeptide compound and application thereof in preparation of antitumor drugs and immunotherapy sensitizer

Resiquimod is delivered specifically to the tumor site through the SR-B1 targeting peptide complex to regulate cholesterol metabolism, solving the problems of the single mechanism of action and immune system disorder of existing PD-L1 inhibitors, and achieving tumor suppression and immunotherapy sensitization effects.

CN120586084APending Publication Date: 2025-09-05HARBIN MEDICAL UNIVERSITY
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Patent Information

Application Number
CN202510781553.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-06-12
Publication Date
2025-09-05

AI Technical Summary

Technical Problem

Existing PD-L1 inhibitors have a single mechanism of action, which leads to insufficient specific enrichment in tumor sites, easily triggers immune system disorders, and has limited therapeutic effects.

Method used

An SR-B1 targeting peptide complex was designed, consisting of an SR-B1 targeting peptide and the Toll-like receptor 7/8 agonist Resiquimod. The hydrophobic part of the SR-B1 targeting peptide aggregated to form nanospherical micelles that encapsulate Resiquimod, achieving tumor-site-specific delivery, activating the immune response, and regulating cholesterol metabolism to inhibit PD-L1 expression.

Benefits of technology

It achieves tumor site-specific drug enrichment, significantly inhibits tumor progression and immunosuppression, enhances tumor immunotherapy sensitivity, improves treatment efficacy and quality of life, and is biosafe.

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Abstract

The invention relates to an SR-B1 targeted polypeptide compound and application thereof in preparation of antitumor drugs and immunotherapy sensitizers, and belongs to the technical field of biological drug manufacturing. In order to solve the problems that an existing PD-L1 inhibitor is single in action mechanism and immune system dysfunction is easily caused, the invention provides an SR-B1 targeted polypeptide compound which is composed of SR-B1 targeted polypeptide and Resiquimod. The SR-B1 targeting polypeptide comprises an SR-B1 targeting peptide fragment, a self-assembly peptide fragment and a hydrophobic molecule which are connected in sequence. The SR-B1 targeting polypeptide can recognize overexpressed SR-B1 in tumor cells, block cholesterol uptake, inhibit tumor progression and inhibit expression of PD-L1 at the same time. The polypeptide compound accurately delivers Resiquimod to a tumor site, anti-tumor immune response is activated, and sensitivity of tumor immunotherapy is greatly enhanced through combination of cholesterol metabolism regulation and immunotherapy.
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