Application of GSK-F1 in preparation of drugs for reducing NSUN2 protein stability, solid tumor targeted therapy and / or radiotherapy sensitization
By developing the small molecule compound GSK-F1 to target and inhibit the NSUN2 protein, the problems of solid tumor growth and radiotherapy resistance have been solved, achieving the effects of tumor growth inhibition and radiosensitization, which has clinical application value.
Patent Information
- Application Number
- CN202511465351.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-10-14
- Publication Date
- 2025-11-11
- Estimated Expiration
- 2045-10-14
AI Technical Summary
In the current technology, the problems of solid tumor growth and radiotherapy resistance caused by high expression of NSUN2 protein have not been effectively solved, and no small molecule inhibitors have been reported in the literature.
The small molecule compound GSK-F1 was developed to reduce the stability of the NSUN2 protein by forming hydrogen bonds with the Val715 and Leu717 residues, thereby targeting and inhibiting the NSUN2 protein. It was then combined with a pharmaceutically acceptable dosage form to prepare targeted therapy and radiosensitizing drugs.
GSK-F1 significantly inhibits the growth of nasopharyngeal carcinoma, breast cancer, lung cancer and liver cancer cells in vitro and in vivo, increases radiosensitivity, has good therapeutic potential and no obvious toxic side effects, and has become a potential NSUN2-targeted anti-tumor drug.