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Discovery of linear unnatural peptides as potent mutant isocitrate dehydrogenase 1 inhibitors by Ugi reaction.

Bioorganic chemistry - 1 Feb 2022

Zhou Xuechen, Zheng Mengzhu, Zhao Na, Hu Yixin, Yang Kaiyin, Huo Junfeng, Liu Guangyuan, Huang Jiangeng, Chen Lixia, Zhou Yirong, Li Hua

Abstract excerpt

Isocitrate dehydrogenases 1 (IDH1) catalyzes the oxidative decarboxylation of isocitrate to ɑ-ketoglutaric acid (α-KG). It is the most frequently mutated metabolic gene in human cancer and its mutations interfere with cell metabolism and epigenetic regulation, thus promoting tumorigenesis. In order to discover potent new mutant IDH1 inhibitors, based on the structure of marketed inhibitor AG-120 (Ivosidenib), we...

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PMID: 34954572
DOI: 10.1016/j.bioorg.2021.105569

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