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KDM2 lysine demethylases: structure, functions, and anticancer targets

Year: 2026

Type: article

Abstract: Post-translational modifications of histones, the protein components of nucleosomes, regulate the local state of chromatin for optimal gene expression. Among these modifications, a balance of methylation and demethylation of particular lysine residues in histones is important, as under physiological conditions this balance provides the permissiveness of chromatin for template processes. An imbalance of methylation and demethylation leads to transcriptional deregulation, a characteristic feature of malignant cells. A specific viewpoint of the authors is a multidisciplinary approach to the analysis of complex and contradictory data on epigenetic regulators. This review presents general information about human histone lysine demethylases (KDM). For the KDM2 subgroup, structural features, mechanism of catalysis (histone demethylation), and the role in tumour biology are considered. Since KDM2 functions are not limited to enzymatic activity, the pharmacological approach for anticancer therapy implies both the design of demethylation blockers, with KDM2 being retained in the cells, and the search for possible tools for total elimination of these proteins. The bibliography includes 174 references.

Source: Russian Chemical Reviews

DOI: 10.59761/rcr5212

Authors: P. M. Osherov, A. V. Kurkin, A. A. Shtil, S. S. Borisevich

Institutions: National Research Nuclear University MEPhI, Lomonosov Moscow State University, Russian Cancer Research Center NN Blokhin, Russian Academy of Sciences, Ufa Institute of Chemistry

Language: English

Topic: Epigenetics and DNA Methylation

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: diamond

OpenAlex ID: W7128820555

FWCI:

Cites: 172

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