Histone Demethylases

Histone demethylases (KDMs) are a family of enzymes that catalyze the removal of methyl groups from lysine and arginine residues on histone tails. They reverse the methylation of lysine and arginine residues that is catalyzed by histone methyltransferases.

The first histone demethylase to be discovered was lysine-specific demethylase 1 (LSD1), but further research identified an additional family of histone demethylases; the Jumonji C domain-containing demethylases (JMJD). JMJDs require both Fe²⁺ and 2-oxoglutarate as co-factors for histone demethylation, whilst the catalysis carried out by LSD1 is dependent on the presence of a protonated nitrogen atom. The JMJD family of demethylases remove methyl groups from tri-methylated histone arginine and lysine residues whereas LSD1 demethylates mono- and di-methylated lysine residues on histone H3 (H3K4 and H3K9), but cannot demethylate tri-methylated residues. To date, only one member of the JMJD family - JMJD6 - has been shown to specifically demethylate arginine residues.

The removal of methyl groups from histone lysine and arginine residues is typically associated with transcriptional repression, but this is not true in all cases; the histone demethylase JMJD2A has recently been shown to function as a transcriptional co-activator of androgen receptor responsive genes.

In addition to co-activation of androgen receptor responsive genes, the biological functions of JMJDs include stem cell self-renewal, the inflammatory response and cell differentiation. JMJD1A has also been shown to be essential during spermatogenesis. LSD1 is also involved in a wide array of biological processes including cell proliferation, chromosome segregation and embryonic development, but more recently has been identified as a potential target for cancer therapeutics.

External sources of pharmacological information for Histone Demethylases :

• BJP Guide

Literature for Histone Demethylases

Tocris offers the following scientific literature for Histone Demethylases to showcase our products. We invite you to request* your copy today!

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Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

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Histone Demethylase Gene Data