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KMID : 0370220210650050344
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Yakhak Hoeji
2021 Volume.65 No. 5 p.344 ~ p.348
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Recent Advances in Development of Glutaminase Inhibitors as Anticancer Agents
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Kim Gyu-Bi
Joo Han-Sol
Jung Jong-Wha
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Abstract
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Glutaminolysis is closely related to uncontrolled tumor growth and metastasis in various glutamine-dependent cancers. As such, rewiring cancer metabolism using a glutaminolysis intervention has attracted much attention with recent progress in developing glutaminase inhibitors as anticancer agents. This review paper described the current understanding of glutaminases and their roles in cancers and small-molecule glutaminase inhibitors. In particular, recent developments of natural and synthetic glutaminase inhibitors were covered, focusing on their binding sites and isoform selectivity and briefly, on their structure?activity relationship. Some of the glutaminase inhibitors are in clinical trials, and if successful, it would lead to novel pharmacological intervention to effectively treat cancers.
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KEYWORD
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Cancer, Glutaminolysis, Glutaminase, Small Molecule Inhibitor, Anticancer Agent
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