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. Author manuscript; available in PMC: 2018 Aug 1.
Published in final edited form as: Mol Cancer Res. 2017 May 8;15(8):1073–1084. doi: 10.1158/1541-7786.MCR-16-0424

Figure 6. Model to summarize the effect of G9a inhibition on USP37 gene expression.

Figure 6

REST and its associated chromatin remodelers including G9a, binds to a RE1 binding site in exon 1 of USP37 gene and represses its expression by di- and tri-methylation of histone H3K9 (orange triangles). From previous studies, USP37 is a p27 specific deubiquitylase, and its loss in REST-expressing medulloblastoma cells leads to p27 degradation and sustained proliferation. Inhibition of REST-associated G9a enzymatic activity by UNC 0638 de-represses USP37 gene expression by blocking histone H3K9 methylation at its promoter, causes an increase in p27 levels and promotes a blockade of tumor growth in mouse intracranial models.