Casein kinase 1α (ck1α) molecular glue degrader
By designing a CK1α molecular gel that combines E3 ubiquitin ligase, we achieved highly efficient and selective degradation of CK1α, which solved the problem of poor degradation effect in existing targeted CK1α treatments and improved the treatment effect on diseases such as prostate cancer and colorectal cancer.
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- GAN & LEE PHARM CO LTD
- Filing Date
- 2025-12-29
- Publication Date
- 2026-07-02
AI Technical Summary
Existing targeted CK1α therapies are ineffective at degrading casein kinase 1α (CK1α), leading to drug resistance and poor treatment outcomes in diseases such as prostate cancer and colorectal cancer.
Develop a CK1α molecular glue that binds to E3 ubiquitin ligase, which induces ubiquitination and degradation of CK1α by binding to E3 ubiquitin ligase. This includes compounds, isomers, isotope derivatives, polymorphs, prodrugs, or pharmaceutically acceptable salts or solvates of the CK1α molecular glue. The structure of the glue is used to alter the conformation of the E3 ligase to achieve targeted degradation.
It achieves highly efficient and selective degradation of CK1α, activates the p53 pathway, induces tumor cell apoptosis and cell cycle arrest, overcomes the drug resistance of tumor cells, has better membrane permeability and blood-brain barrier penetration ability, and improves the therapeutic effect on diseases such as prostate cancer and colorectal cancer.
Smart Images
Figure CN2025146824_02072026_PF_FP_ABST