Patenting perspective on Keap1 inhibitors (2019-2024)

被引：0
|
作者：
Luo, Yongfu [1 ]
Yang, Ziyu [1 ]
Zhang, Yuan [1 ]
Jiang, Shutong [1 ]
Zhu, Jingyu [1 ]
Li, Xiangyang [1 ,2 ]
You, Qidong [1 ,3 ,4 ,5 ]
Lu, Mengchen [1 ]
机构：
[1] Soochow Univ, Coll Pharmaceut Sci, Med Coll, Dept Med Chem, Suzhou 215123, Peoples R China
[2] Microcell Pharmaceut Suzhou Co Ltd, Dept Res & Dev, Suzhou, Peoples R China
[3] China Pharmaceut Univ, Jiangsu Key Lab Drug Design & Optimizat, TongJiaXiang 24, Nanjing 210009, Peoples R China
[4] China Pharmaceut Univ, State Key Lab Nat Med, TongJiaXiang 24, Nanjing 210009, Peoples R China
[5] China Pharmaceut Univ, Nanjing 211198, Peoples R China
来源：
EXPERT OPINION ON THERAPEUTIC PATENTS | 2025年 / 35卷 / 04期
基金：
中国国家自然科学基金;
关键词：
Keap1; Nrf2; oxidative stress; electrophilic inhibitors; protein-protein interaction inhibitors; PROTEIN-PROTEIN INTERACTION; FUMARIC-ACID ESTERS; OXIDATIVE STRESS; DIMETHYL FUMARATE; MULTIPLE-SCLEROSIS; KELCH DOMAIN; NRF2; PATHWAY; ACTIVATION; BINDING; REDOX;
D O I：
10.1080/13543776.2025.2462844
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
IntroductionKelch-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 coveredThis 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 opinionExtensive 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.
引用
收藏
页码：325 / 356
页数：32
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