ASH1L degrading agent and treatment method using the same

JP7789402B2Active Publication Date: 2025-12-22THE RGT UNIV OF MICHIGAN
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Patent Information

Application Number
JP2024002472
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2017-11-10
Filing Date
2024-01-11
Publication Date
2025-12-22
Estimated Expiration
2038-11-09

AI Technical Summary

Technical Problem

Current treatments for diseases associated with ASH1L activity, such as acute leukemia and solid cancers, lack effective methods to target and degrade ASH1L, a histone-lysine N-methyltransferase implicated in oncogenic transformation and overexpression in various tumors.

Method used

Development of ASH1L-targeted proteolysis-targeted chimeras (PROTACs) comprising a domain that binds to ASH1L and a second domain that promotes its degradation, utilizing ubiquitin ligases like cereblon or von Hippel-Lindau E3 ligase.

Benefits of technology

The compounds effectively inhibit and degrade ASH1L, offering potential therapeutic benefits for diseases dependent on ASH1L activity, including acute leukemia and solid cancers.

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Patent Text Reader

Abstract

To provide methods for treatment of a disease dependent on activity of ASH1L.SOLUTION: There are provided herein small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for treatment of a disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.SELECTED DRAWING: Figure 1
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Citation Information

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