EHMT2/G9a as an Epigenetic Target in Pediatric and Adult Brain Tumors |
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| Authors: | Barbara Kunzler Souza Natalia Hogetop Freire Mariane Jaeger Caroline Brunetto de Farias Algemir L Brunetto Andr T Brunetto Rafael Roesler |
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| Affiliation: | 1.Cancer and Neurobiology Laboratory, Experimental Research Center, Clinical Hospital (CPE-HCPA), Federal University of Rio Grande do Sul, Porto Alegre 90035-003, Brazil; (N.H.F.); (M.J.); (C.B.d.F.); (A.L.B.); (A.T.B.);2.Epigenica Biosciences, Canoas 92035-000, Brazil;3.Children’s Cancer Institute, Porto Alegre 90620-110, Brazil;4.Department of Pharmacology, Institute for Basic Health Sciences, Federal University of Rio Grande do Sul, Porto Alegre 90050-170, Brazil |
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| Abstract: | Epigenetic mechanisms, including post-translational modifications of DNA and histones that influence chromatin structure, regulate gene expression during normal development and are also involved in carcinogenesis and cancer progression. The histone methyltransferase G9a (euchromatic histone lysine methyltransferase 2, EHMT2), which mostly mediates mono- and dimethylation by histone H3 lysine 9 (H3K9), influences gene expression involved in embryonic development and tissue differentiation. Overexpression of G9a has been observed in several cancer types, and different classes of G9a inhibitors have been developed as potential anticancer agents. Here, we review the emerging evidence suggesting the involvement of changes in G9a activity in brain tumors, namely glioblastoma (GBM), the main type of primary malignant brain cancer in adults, and medulloblastoma (MB), the most common type of malignant brain cancer in children. We also discuss the role of G9a in neuroblastoma (NB) and the drug development of G9a inhibitors. |
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| Keywords: | G9a EHMT2 glioblastoma medulloblastoma epigenetics brain tumor |
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