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Comprehensive exploration of isocitrate dehydrogenase (IDH) mutations: Tumorigenesis, drug discovery, and covalent inhibitor advances.

European journal of medicinal chemistry - 15 Jan 2025

Gai Conghao, Zeng Hairong, Xu Haoming, Chai Xiaoyun, Zou Yan, Zhuang Chunlin, Ge Guangbo, Zhao Qingjie

Abstract excerpt

Isocitrate dehydrogenase (IDH) is an enzyme that catalyses the oxidative decarboxylation of isocitrate, producing α-ketoglutarate (α-KG) relative to the hydroxylation of substrates. However, IDH mutants can further reduce α-KG to 2-hydroxyglutarate (2-HG) which competitively inhibits α-KG dependent enzymes, leading to the downregulation of normal hydroxylation pathways. Good IDH mutant inhibitors can effectively...

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PMID: 39591851
DOI: 10.1016/j.ejmech.2024.117041

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