Novel compound as UCHL-5 inhibitor and uses thereof

Novel pyrazine and quinoxaline derivatives target UCHL-5 to overcome bortezomib resistance, inducing endoplasmic reticulum stress and apoptosis in cancer cells, providing effective treatment for bortezomib-resistant multiple myeloma and colon cancer.

WO2026024060A1 Publication Date: 2026-01-29KOREA RES INST OF BIOSCIENCE & BIOTECHNOLOGY +1
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Patent Information

Application Number
PCT/KR2025/010814
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2025-07-21
Filing Date
2025-07-22
Publication Date
2026-01-29

AI Technical Summary

Technical Problem

Existing proteasome inhibitors like bortezomib face challenges with membrane impermeability and cancer cell resistance, limiting their therapeutic efficacy against UCHL-5 mediated diseases such as multiple myeloma and other cancers.

Method used

Development of novel pyrazine and quinoxaline derivative compounds that inhibit UCHL-5 activity, leading to ubiquitinated protein accumulation and endoplasmic reticulum stress in cancer cells, effectively targeting bortezomib-resistant cancers.

Benefits of technology

The compounds induce apoptosis in cancer cells by inhibiting UCHL-5, demonstrating anticancer activity even in bortezomib-resistant cancers, including multiple myeloma and colon cancer, and inhibit ubiquitin-proteasome system activity.

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Abstract

The present invention relates to a novel compound as an ubiquitin C-terminal hydrolase L5 (UCHL -5) inhibitor and uses thereof.
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