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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

Isocitrate Dehydrogenase 2 Inhibitors for the Treatment of Hematologic Malignancies: Advances and Future Opportunities

Author(s): Feng Huang, Tian Tian, Yizhe Wu, Jinxin Che, Haiyan Yang* and Xiaowu Dong*

Volume 21 , Issue 9 , 2021

Published on: 30 November, 2020

Page: [1113 - 1122] Pages: 10

DOI: 10.2174/1389557520666201130102724

Price: $65


Tumor cells frequently reprogram cellular metabolism from oxidative phosphorylation to glycolysis. Isocitrate dehydrogenase 2 (IDH2) has been intensively studied due to its involvement in the metabolic activity of cancer cells. Mutations in IDH2 promote neomorphic activity through the generation of oncometabolite 2-hydroxyglutarate (2-HG). The overproduced 2-HG can competitively inhibit α-KG-dependent dioxygenases to trigger cell differentiation disorders, a major cause of blood tumors. This review outlines recent progress in the identification of IDH2 inhibitors in blood cancer to provide a reference for ongoing and future clinical studies.

Keywords: Isocitrate dehydrogenase 2, IDH2, mutant, inhibitors, structure-activity relationship, blood cancer.

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