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Literature DB >> 16408017

Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.

Dorothea Greiner¹, Tiziana Bonaldi, Ragnhild Eskeland, Ernst Roemer, Axel Imhof.

Abstract

Histone methylation plays a key role in establishing and maintaining stable gene expression patterns during cellular differentiation and embryonic development. Here, we report the characterization of the fungal metabolite chaetocin as the first inhibitor of a lysine-specific histone methyltransferase. Chaetocin is specific for the methyltransferase SU(VAR)3-9 both in vitro and in vivo and may therefore be used to study heterochromatin-mediated gene repression.

Entities: Chemical

Mesh：

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Year: 2005 PMID： 16408017 DOI： 10.1038/nchembio721

Source DB: PubMed Journal: Nat Chem Biol ISSN： 1552-4450 Impact factor: 15.040

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Cited

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Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.

1. A practical sulfenylation of 2,5-diketopiperazines.

Review 2. Epigenetic protein families: a new frontier for drug discovery.

Review 3. Chemical and biochemical approaches in the study of histone methylation and demethylation.

4. Efficient cell migration requires global chromatin condensation.

5. General approach to epipolythiodiketopiperazine alkaloids: total synthesis of (+)-chaetocins A and C and (+)-12,12'-dideoxychetracin A.

6. PRMT1 methylates the single Argonaute of Toxoplasma gondii and is important for the recruitment of Tudor nuclease for target RNA cleavage by antisense guide RNA.

Review 7. Epigenetic regulation of epithelial-mesenchymal transition.

Review 8. Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases.

Review 9. Epidithiodioxopiperazines. occurrence, synthesis and biogenesis.

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