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. 2020 May 22;10:8567. doi: 10.1038/s41598-020-65593-x

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© The Author(s) 2020

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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PBB153 decreases DNA methyltransferase activity during spermatogenesis and binds to the active site of DNMT3A. (A). De novo DNMT activity was measured in response to three PBB153 doses during in vitro differentiation of hESCs. De novo DNMT activity decreased significantly for all three PBB153 doses. (B). De novo DNMT activity of DMSO control was measured in response to direct PBB153 treatment (10 µM) and significantly decreased. (C). Maintenance DNMT activity was measured in response to three PBB153 doses during the in vitro differentiation of hESCs. Maintenance DNMT activity significantly decreased in response to the 500 nM PBB153 dose. (D). Maintenance DNMT activity of DMSO control was measured in response to direct PBB153 treatment and significantly decreased. For each, significance determined by a one-tailed-independent t-test and designated by asterisks where *is p < 0.05; **is p < 0.01; ***is p < 0.001 and n.s. is no significance compared to DMSO control (p > 0.05). In the box plots shown in (A–D), centerlines represent the medians and box limits indicate the 25^th and 75^th percentiles which were calculated by R software; the extent of the whiskers represent 1.5 times the interquartile range from the 25^th and 75^th percentiles. Outliers are shown as data points outside of the whisker range. (E). Structure of PBB153. (F). Docking of PBB153 in the active site of DNA methyltransferase 3 A (PDB: 2qrv) using Achilles Blind Docking Server. PBB153 potentially interacts with amino acids in the active site and inhibits DNMT 3 A/3B from catalyzing DNA methylation reactions. The purple dashed line indicates a pi-cation interaction. The green dashed lines indicate hydrophobic interactions. The orange dashed line indicates a halogen bond. (G). Docking of PBB153 in the active site of DNA methyltransferase 1 (PDB: 4wxx) using Achilles Blind Docking Server. PBB153 potentially interacts with amino acids in the active site and inhibits DNMT 1 from catalyzing DNA methylation reactions. The purple dashed line indicates a pi-cation interaction. The green dashed line indicates a hydrophobic interaction. Orange dashed lines indicate halogen bonds.