Functional role of G9a histone methyltransferase in cancer

Casciello, Francesco, Windloch, Karolina, Gannon, Frank and Lee, Jason S. (2015) Functional role of G9a histone methyltransferase in cancer. Frontiers in Immunology, 6 SEP: 487.1-487.12. doi:10.3389/fimmu.2015.00487

Author Casciello, Francesco
Windloch, Karolina
Gannon, Frank
Lee, Jason S.
Title Functional role of G9a histone methyltransferase in cancer
Journal name Frontiers in Immunology   Check publisher's open access policy
ISSN 1664-3224
Publication date 2015-09-25
Sub-type Article (original research)
DOI 10.3389/fimmu.2015.00487
Open Access Status DOI
Volume 6
Issue SEP
Start page 487.1
End page 487.12
Total pages 12
Place of publication Lausanne, Switzerland
Publisher Frontiers Research Foundation
Language eng
Formatted abstract
Post-translational modifications of DNA and histones are epigenetic mechanisms, which affect the chromatin structure, ultimately leading to gene expression changes. A number of different epigenetic enzymes are actively involved in the addition or the removal of various covalent modifications, which include acetylation, methylation, phosphorylation, ubiquitination, and sumoylation. Deregulation of these processes is a hallmark of cancer. For instance, G9a, a histone methyltransferase responsible for histone H3 lysine 9 (H3K9) mono- and dimethylation, has been observed to be upregulated in different types of cancer and its overexpression has been associated with poor prognosis. Key roles played by these enzymes in various diseases have led to the hypothesis that these molecules represent valuable targets for future therapies. Several small molecule inhibitors have been developed to specifically block the epigenetic activity of these enzymes, representing promising therapeutic tools in the treatment of human malignancies, such as cancer. In this review, the role of one of these epigenetic enzymes, G9a, is discussed, focusing on its functional role in regulating gene expression as well as its implications in cancer initiation and progression. We also discuss important findings from recent studies using epigenetic inhibitors in cell systems in vitro as well as experimental tumor growth and metastasis assays in vivo.
Keyword G9a
Epigenetic regulation
Histone methylation
Tumor growth
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
School of Chemistry and Molecular Biosciences
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Created: Fri, 09 Oct 2015, 20:26:30 EST by Mrs Louise Nimwegen on behalf of School of Chemistry & Molecular Biosciences