A near-infrared fluorescent diagnostic and therapeutic probe capable of real-time monitoring of ERα protein degradation, and its preparation method and application
By designing and synthesizing near-infrared fluorescence diagnostic and treatment probes that can monitor ERα protein degradation in real time, the problem of inaccurate monitoring of ERα protein in breast cancer treatment is solved, real-time monitoring and efficient degradation of ERα protein is achieved, and the treatment effect and accuracy are improved.
Patent Information
- Application Number
- CN202311647151.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2023-12-04
- Publication Date
- 2025-08-15
- Estimated Expiration
- 2043-12-04
AI Technical Summary
The existing breast cancer treatment methods lack precise monitoring and real-time monitoring methods for ERα protein, resulting in poor treatment results.
A near-infrared fluorescence diagnostic and treatment probe that can monitor the degradation of ERα protein in real time was designed. A series of near-infrared fluorescence diagnostic and treatment probes were synthesized using a highly ERα-targeted fluorophore 2-(6-hydroxy-2-(4-hydroxystyrene)-4H-benzopyran-4-subunit)malonitrile, a highly ERα-targeted fluorophore, was used as a warhead for specifically binding to the target protein. Methyl VHL was used as a ligand to recruit E3 ligase, and carbon chains of different lengths were used as linkers to synthesize a series of near-infrared fluorescence diagnostic and treatment probes.
Real-time monitoring and efficient degradation of ERα protein are achieved, the accuracy and effectiveness of breast cancer treatment are improved, excellent anti-proliferative activity, and near-infrared visualization performance.