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Article

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.

EMBO reports - 1 May 2011

Chowdhury Rasheduzzaman, Yeoh Kar Kheng, Tian Ya-Min, Hillringhaus Lars, Bagg Eleanor A, Rose Nathan R, Leung Ivanhoe K H, Li Xuan S, Woon Esther C Y, Yang Ming, McDonough Michael A, King Oliver N, Clifton Ian J, Klose Robert J, Claridge Timothy D W, Ratcliffe Peter J, Schofield Christopher J, Kawamura Akane

Abstract excerpt

Mutations in isocitrate dehydrogenases (IDHs) have a gain-of-function effect leading to R(-)-2-hydroxyglutarate (R-2HG) accumulation. By using biochemical, structural and cellular assays, we show that either or both R- and S-2HG inhibit 2-oxoglutarate (2OG)-dependent oxygenases with varying potencies. Half-maximal inhibitory concentration (IC(50)) values for the R-form of 2HG varied from approximately 25 μM for...

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Identifiers

PMID: 21460794
DOI: 10.1038/embor.2011.43
PMCID: PMC3090014

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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