A compound that degrades Polθ based on a hydrophobic tag, its preparation method and uses
By designing compounds based on a hydrophobic tag degradation strategy, the problem of difficulty in targeting upregulated Polθ protein expression in existing technologies has been solved, achieving efficient degradation of Polθ protein and providing a new drug target for treating homologous recombination-deficient cancers, especially for the treatment of various cancers such as breast cancer.
CN119823115BActive Publication Date: 2026-05-26CHINA PHARM UNIV
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- CHINA PHARM UNIV
- Filing Date
- 2025-01-06
- Publication Date
- 2026-05-26
AI Technical Summary
Technical Problem
Current technologies are unable to effectively target and treat upregulated Polθ proteins, resulting in an inability to effectively treat cancers with homologous recombination defects.
Method used
A series of compounds or their pharmaceutically acceptable salts were designed and synthesized using a hydrophobic tag-based degradation strategy. These compounds were then specifically bound to and degraded by the Polθ protein, and the degradation efficiency was enhanced using PROTAC technology.
Benefits of technology
This study achieved efficient degradation of the Polθ protein, providing a novel drug target for treating homologous recombination-deficient cancers, particularly breast cancer and other cancers.
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Figure CN119823115B_ABST
Abstract
This invention discloses a compound that degrades Polθ based on a hydrophobic tag, its preparation method, and its uses. The structural formula of the compound that targets and degrades Polθ is shown in general formula (I). Compared with Polθ inhibitors, the compound of this invention can degrade the Polθ protein at appropriate doses.
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