G9a-like protein (human recombinant)

Post-translational modification of histones by methylation of lysine residues can promote transcriptional activation or repression. G9a-like protein (GLP) and G9a are SET domain-containing methyltransferases that specifically mono- and di-methylate histone H3 at lysine 9 (H3K9).^1,2 Methylation of H3K9 by a GLP/G9a heteromeric complex regulates gene expression by silencing euchromatin.³ GLP and G9a share 80% sequence identity in their SET domains. Structure-activity relationship (SAR) studies have been employed to design potent and selective inhibitors of these proteins, including BIX-01294 and UNC0638, with IC₅₀ values in the nanomolar range.⁴

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1. Wu, H., Min, J., Lunin, V.V., et al. Structural biology of human H3K9 methyltransferases. PLoS One 5(1), e8570 (2010).

2. Patnaik, D., Chin, H.G., Estève, P.O., et al. Substrate specificity and kinetic mechanism of mammalian G9a histone H3 methyltransferase. The Journal of Biological Chemisty 279(51), 53248-53258 (2004).

3. Tachibana, M., Matsumura, Y., Fukuda, M., et al. G9a/GLP complexes independently mediate H3K9 and DNA methylation to silence transcription. EMBO J. 27(20), 2681-2690 (2008).

4. Chang, Y., Zhang, X., Horton, J.R., et al. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat. Struct. Mol. Biol. 16(3), 312-317 (2009).