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. 2019 Jan 3;10:19. doi: 10.1038/s41467-018-07905-4

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© The Author(s) 2019

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Fig. 2 — Structural mechanisms of PMT inhibition by chemical probes. a Inhibitors of G9a (PDB: 3HNA (GLP with H3K9 substrate) and 4NVQ (A-366)); SUV420H2 (PDB: 4AU7 (mSUV420H2 with H4 substrate) and SUV420H1 (PDB: 5CPR (A-196)); SETD7 (PDB: 1O9S (H3 substrate) and 4JLG (PFI-2)); PRMT5 (PDB: 4GQB (H4 substrate) and 5C9Z (GSK591)); SMYD2 (PDB: 3TG5 (p53 substrate) and 5ARG (BAY-598)); SMYD3 (PDB: 5EX0 (MAP3K2 substrate) and (BAY-6035)) all bind in the substrate (peptide) binding pocket. b SGC0946 binds in the SAM-binding pocket of DOT1L thereby preventing cofactor binding (PDB ID: 3QOW (SAM), 4ER6 (SGC0946)). LLY-283 also occupies the SAM-binding pocket of PRMT5-MEP50 complex (PDB ID: 4GQB (SAM analog) and 6CKC (LLY-283)). c Three distinct modes of allosteric inhibition of protein methyltransferases. SGC707 binds to PRMT3 in an allosteric site that prevents productive formation of the enzyme’s activation helix (PDB ID: 4RYL). OICR-9429 binds to WDR5 and inhibits MLL1 activity by disrupting WDR5-MLL1-RBBP5 complex (PDB ID: 4QL1). A-395 binds to the EED subunit of the PRC2 complex thereby preventing binding of activating peptides (PDB ID: 5K0M)