Histone demethylation mediated by the nuclear amine oxidase...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/26 (2006.01)

Patent

CA 2591717

LSD1, a homolog of nuclear amine oxidases, functions as a histone demethylase and transcriptional co-repressor. LSD1 specifically demethylates histone H3 lysine 4, which is linked to active transcription. Lysine demethylation occurs via an oxidation reaction that generates formaldehyde. Importantly, RNAi inhibition of LSD1 causes an increase in H3 lysine 4 methylation and concomitant de-repression of target genes, suggesting that LSD1 represses transcription via histone demethylation. The results thus identify a histone demethylase conserved from S. pombe to human and reveal dynamic regulation of histone methylation by both histone methylases and demethylases.

LSD1, un homologue d'oxydases d'amine nucléaires, fonctionne comme une déméthylase d'histone et co-répresseur transcriptionnel. LSD1 déméthyle spécifiquement la lysine 4 de l'histone H3, qui est lié à la transcription active. La déméthylation de la lysine intervient via une réaction d'oxydation qui produit du formaldéhyde. L'important, c'est que l'inhibition par l'ARN interférence du LSD1 provoque une augmentation de la méthylation de la lysine 4 du H3, et une dé-répression concomitante des gènes cibles, ce qui donne à penser que le LSD1 réprime la transcription via déméthylation de l'histone. Le résultat identifie ainsi une déméthylase d'histone conservée de S. pombe jusqu'à l'humain et fait apparaître une régulation dynamique de la méthylation de l'histone tant par les méthylases que les déméthylases de l'histone.

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