Ether-À-go-go 1 (EAG1) potassium channel inhibitors and uses thereof

Selective small molecule inhibitors targeting the PAS domain of EAG1 channels address the issue of off-target effects, offering effective treatment for neurological disorders and cancer by modulating potassium channel activity.

WO2026128764A1 Publication Date: 2026-06-18GEORGETOWN UNIV
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
GEORGETOWN UNIV
Filing Date
2025-12-11
Publication Date
2026-06-18

AI Technical Summary

⚠Technical Problem

Existing small molecule inhibitors for Ether-a-go-go (EAG) potassium channels suffer from non-specific binding, leading to off-target effects and limited efficacy in treating neurological disorders and cancer, particularly due to their interaction with the Per-Amt-Sim (PAS) domain.

⚗Method used

Development of small molecule inhibitors that selectively bind to the PAS domain of EAG1 channels, utilizing polycyclic compounds with unsaturated rings and pendent substituents to modulate potassium channel activity, thereby reducing off-target effects.

🎯Benefits of technology

The selective inhibitors effectively target EAG1 channels, providing therapeutic benefits for neurological disorders and cancer by modulating potassium channel activity while minimizing adverse effects on other cellular functions.

✦ Generated by Eureka AI based on patent content.

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Abstract

The disclosure provides methods for the treatment of disorders associated with an increase in potassium channel activity using small molecule inhibitors, such as compounds that selectively bind to a Per-Arnt-Sim (PAS) domain of Ether-à-go-go 1 (EAG1) potassium channels. The disclosure also features pharmaceutical compositions comprising therapeutically effective amounts of the disclosed small molecule inhibitors.
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