Transducin beta-like protein 1 degraders

WO2024206100A3PCT designated stage expired Publication Date: 2024-12-26OHIO STATE INNOVATION FOUND
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Patent Information

Application Number
PCT/US2024/021053
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-03-24
Filing Date
2024-03-22
Publication Date
2024-12-26

AI Technical Summary

Technical Problem

Current PROTAC compounds, such as tegavivint, have limitations in effectively targeting and degrading Transducin β-like protein 1 X-linked (TBL1X) for the treatment of proliferative disorders like cancer, particularly in modulating the Wnt/β-catenin pathway, necessitating the development of improved systems and methods for targeting TBL1X.

Method used

Development of novel PROTAC compounds with a tegavivint warhead covalently linked to an E3 ligase ligand, utilizing a linker to simultaneously engage TBL1X and the E3 ligase for ubiquitination and subsequent proteasomal degradation, enhancing therapeutic efficacy against TBL1X-related cancers.

Benefits of technology

The new PROTAC compounds demonstrate enhanced ability to promote apoptosis in Wnt-driven cancers by disrupting TBL1X/β-catenin interactions, offering improved therapeutic effects compared to existing compounds.

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Abstract

Disclosed herein are transducin β-like protein 1 X-linked targeting compounds covalently linked to an E3 ligase ligand. The compounds are useful for the treatment of cancer.
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Citation Information

Patent Citations

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