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Patenting perspective on Keap1 inhibitors (2019-2024)

Yongfu Luo¹, Ziyu Yang¹, Yuan Zhang¹

¹Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University Medical College, Suzhou, China.

Expert Opinion on Therapeutic Patents

|February 5, 2025

Abstract

Introduction:

Kelch-like ECH-associated protein 1 (Keap1), an E3 ligase negatively regulating the nuclear factor erythroid 2-related factor 2 (Nrf2), has emerged as an auspicious drug target for treating ailments associated with oxidative stress and inflammation. Discovery of Keap1 inhibitors have attracted significant interest.

Areas Covered:

This review covers patents on Keap1 inhibitors from 2019 to 2024, providing a comprehensive analysis of their structural characteristics, optimization strategies, pharmacological properties and clinical progress.

Expert Opinion:

Extensive efforts have been devoted to enhance potency and drug-like properties of Keap1 inhibitors. Strategies such as ROS-cleavable prodrug design, bivalent inhibition and PROTACs are emerging. As the range of drug types and applications expands, Keap1 inhibitors are becoming a sagacious option for disease treating.

Keywords:

Keap1 Nrf2 electrophilic inhibitors oxidative stress protein-protein interaction inhibitors

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