Protein degradation targeting chimera targeting stat3 and preparation method and medical use thereof

By designing protein degradation-targeting chimeras (PROTACs) targeting STAT3, the problems of poor selectivity and high toxicity of existing STAT3 inhibitors have been solved, achieving effective degradation of STAT3 protein and inhibition of tumor cells.

CN118026997BActive Publication Date: 2026-06-09CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHINA PHARM UNIV
Filing Date
2024-02-19
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing STAT3 inhibitors suffer from poor selectivity, high toxicity, and low bioavailability. Furthermore, inhibiting STAT3 protein expression can lead to cellular drug resistance. Therefore, there is a need to develop a novel drug that can effectively degrade STAT3 protein.

Method used

Protein degradation targeting chimeras (PROTACs) targeting STAT3 were designed. By catalyzing the formation of a complex between the target protein and E3 ubiquitin ligase, STAT3 ubiquitination and proteasome degradation are achieved, thereby reducing the expression level of STAT3.

Benefits of technology

It significantly degrades the target protein STAT3, exhibits low toxicity and high bioavailability, and can effectively inhibit tumor cell proliferation, showing potential as an anti-tumor drug.

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Abstract

The application discloses a compound with a structure as shown in formula I or a pharmaceutically acceptable salt thereof, wherein L is selected from n1 is an integer from 2 to 7, n2 is an integer from 1 to 4, n3 is an integer from 4 to 6, and R is selected from the application. The compound only needs a small amount of use to have a significant cell proliferation inhibiting effect on tumor cells, can significantly degrade target proteins STAT3 and pSTAT3, can degrade STAT3 through a ubiquitin-proteasome pathway, and has almost no influence on STAT1 and STAT2. The application further discloses a use of the compound or the pharmaceutically acceptable salt thereof in preparation of a STAT3 degradation targeting agent.
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