A cdK4 proteolysis targeting chimera, and preparation method and application thereof
CN122325451APending Publication Date: 2026-07-03BEIJING GUOHAOYU MEDICAL TECH CO LTD +1
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Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- BEIJING GUOHAOYU MEDICAL TECH CO LTD
- Filing Date
- 2026-04-22
- Publication Date
- 2026-07-03
AI Technical Summary
Technical Problem
The lack of suitable CDK4 ligands and E3 ligase ligands in current technologies limits the development of CDK4 proteolytic targeting chimeras in the field of tumor therapy.
Method used
A specific chemical synthesis procedure was used to synthesize a CDK4 protein hydrolysis-targeting chimera, including the preparation of intermediate 1, compound A and intermediate 2, and finally the combination with peducolic acid to form a chimera containing an E3 ubiquitin ligase ligand and a target protein ligand.
Benefits of technology
It achieved specific degradation of CDK4 protein, enhancing the in vivo anti-tumor effect, especially showing significant anti-proliferative activity and tumor inhibition rate in the treatment of colorectal cancer and lung cancer.
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Figure CN122325451A_ABST
Abstract
This invention relates to the field of pharmaceutical technology, and more particularly to a CDK4 protein hydrolysis-targeting chimera, its preparation method, and its applications. The structural formula of the CDK4 protein hydrolysis-targeting chimera is as follows: The CDK4 protein hydrolysis-targeting chimera comprises an E3 ubiquitin ligand compound A, a target protein ligand peducolic acid, and an ester linker arm connecting the two active ligands, exhibiting excellent in vivo antitumor effects.
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