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. 2016 Aug 19;6:29176. doi: 10.1038/srep29176

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Copyright © 2016, The Author(s)

This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/

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(A) EPZ005687, a strong inhibitor of EZH2, enhanced the activity of SFRP1 in human OA chondrocytes shown by Realtime PCR. (B) EPZ005687 revived the inhibited SFRP1 in OA chondrocytes shown by Westernblot. (C) EPZ005687 delayed OA development demonstrated by SO staining. Scale bars, 200 & 50 μm. (D) OARSI scoring of OA severity upon EPZ005687 treatment. The in vivo experiments clearly demonstrated the therapeutic effects of EPZ005687 on OA cartilage degeneration in mice. (E–J) The cartilage samples from sham, OA + EZP205687 and OA + NS group were examined for the expression of COLX, ADAMTS-5, MMP3, MMP13, SFRP1 and β-catenin by Realtime PCR. The results confirmed the protective effect of EPZ005687 on chondrocytes. Values are means ± SD (n = 3). *p < 0.05, **p < 0.01.