Bifunctional compounds for targeting pkmyt1 and methods of use
Patent Information
- Authority / Receiving Office
- EP · EP
- Patent Type
- Applications
- Current Assignee / Owner
- INSILICO MEDICINE IP LTD
- Filing Date
- 2024-08-22
- Publication Date
- 2026-07-01
AI Technical Summary
There is a need for effective treatments for diseases and conditions related to PKMYT1 regulation or activity, such as cancer, as existing therapies are inadequate in targeting this specific pathway.
A bifunctional compound with a chemical structure of ULM―L―PTM, where PTM is a small molecule comprising a PKMYT1 protein targeting moiety, ULM is a small molecule E3 ubiquitin ligase binding moiety, and L is a bond or chemical linking moiety, is developed to modulate PKMYT1 activity by inducing its degradation through the ubiquitin-proteasome pathway.
The bifunctional compound effectively inhibits PKMYT1 and potentially other targets like WEE1, leading to therapeutic benefits in reducing tumor proliferation and overcoming drug resistance, thereby providing a novel approach for treating PKMYT1-associated disorders.
Smart Images
Figure PCTCN2024113808-FTAPPB-I100001 
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Figure PCTCN2024113808-FTAPPB-I100003