KRAS-protac chimeric compound and use thereof
By developing KRAS-PROTAC chimeric compounds, PROTAC technology is used to induce the degradation of KRAS protein, the problem of difficulty in targeted treatment of cancer caused by KRAS gene mutations is solved, and effective inhibition and degradation of KRAS mutants are achieved.
WO2025061079A1 Publication Date: 2025-03-27HANGZHOU ZHONGMEI HUADONG PHARMACEUTICAL CO LTD
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Patent Information
- Application Number
- PCT/CN2024/119593
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-03-28
- Filing Date
- 2024-09-19
- Publication Date
- 2025-03-27
AI Technical Summary
Technical Problem
KRAS gene mutations, especially KRASG12D, cause cancers that are difficult to target, because the surface of KRAS protein is "smooth" and difficult to target, resulting in KRAS being cursed that "unprepared" and "no medicine to target".
Method used
Developed KRAS-PROTAC chimeric compounds that induce the degradation of KRAS protein by binding to ligands of KRAS ligands and E3 ligase to achieve targeted treatment of KRAS mutants.
Benefits of technology
Effectively inhibiting and degrading KRAS G12D mutant proteins provide a potential new way to treat diseases such as tumors, overcoming the limitations of traditional small-molecule drugs that are difficult to target KRAS.
✦ Generated by Eureka AI based on patent content.
Abstract
Provided are a compound represented by [B-L]n-KRAS ligand (I) or a pharmaceutically acceptable salt or stereoisomer thereof, and a use thereof in treating diseases such as tumor diseases, immune diseases or inflammatory diseases. Also provided are a pharmaceutical formulation and pharmaceutical composition comprising the compound, and a use thereof.
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