Bifunctional molecular compound for inducing SHP2 protein degradation based on DCAF16 ligand as well as preparation method and application of bifunctional molecular compound
By developing a bifunctional molecular compound based on DCAF16 ligand to target and degrade SHP2 protein, the shortcomings of existing technologies in targeting and degrading SHP2 protein were overcome. This resulted in low-micromolar levels of anti-proliferation and anti-tumor effects in HeLa cells, restoring the anti-tumor immune function of T cells.
CN122059932APending Publication Date: 2026-05-19FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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Patent Information
- Application Number
- CN202610158217.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-02-04
- Publication Date
- 2026-05-19
AI Technical Summary
Technical Problem
Current technologies lack effective methods to target and degrade the SHP2 protein, resulting in an inability to effectively inhibit various cancers and restore the anti-tumor immune function of T cells.
Method used
We developed bifunctional molecular compounds KB02 and SHP099 based on DCAF16 ligands as target protein ligands, and linked them through different linkers to form PROTACs compounds that can target and degrade SHP2 protein.
Benefits of technology
These compounds exhibited potent antiproliferative activity in HeLa cells, inducing SHP2 degradation at low micromolar levels, inhibiting tumor cell growth, and restoring T cell anti-tumor immune function, demonstrating deep inhibition of the RAS/MAPK and PI3K/AKT/mTOR pathways.
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Abstract
The invention discloses a bifunctional molecule compound for inducing SHP2 protein degradation based on a DCAF16 ligand as well as a preparation method and application of the bifunctional molecule compound, belongs to the technical field of medicines, and relates to a bifunctional molecule for inducing SHP2 protein degradation based on the DCAF16 ligand as shown in a general formula (I) or pharmaceutically acceptable salt of the bifunctional molecule, and a pharmaceutical composition containing an SHP2 protein targeted degradation agent. The invention also relates to a preparation method of the compound and application of the compound in preparation of medicines for treating SHP2-mediated tumors and / or other diseases.
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