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Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.
Qi W, Chan H, Teng L, Li L, Chuai S, Zhang R, Zeng J, Li M, Fan H, Lin Y, Gu J, Ardayfio O, Zhang JH, Yan X, Fang J, Mi Y, Zhang M, Zhou T, Feng G, Chen Z, Li G, Yang T, Zhao K, Liu X, Yu Z, Lu CX, Atadja P, Li E. Qi W, et al. Among authors: zhao k. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5. doi: 10.1073/pnas.1210371110. Epub 2012 Dec 10. Proc Natl Acad Sci U S A. 2012. PMID: 23236167 Free PMC article.
Histone methylation by PRC2 is inhibited by active chromatin marks.
Schmitges FW, Prusty AB, Faty M, Stützer A, Lingaraju GM, Aiwazian J, Sack R, Hess D, Li L, Zhou S, Bunker RD, Wirth U, Bouwmeester T, Bauer A, Ly-Hartig N, Zhao K, Chan H, Gu J, Gut H, Fischle W, Müller J, Thomä NH. Schmitges FW, et al. Among authors: zhao k. Mol Cell. 2011 May 6;42(3):330-41. doi: 10.1016/j.molcel.2011.03.025. Mol Cell. 2011. PMID: 21549310 Free article.
Detecting S-adenosyl-L-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay.
Lin Y, Fan H, Frederiksen M, Zhao K, Jiang L, Wang Z, Zhou S, Guo W, Gao J, Li S, Harrington E, Meier P, Scheufler C, Xu YC, Atadja P, Lu C, Li E, Gu XJ. Lin Y, et al. Among authors: zhao k. Anal Biochem. 2012 Apr 1;423(1):171-7. doi: 10.1016/j.ab.2012.01.019. Epub 2012 Jan 27. Anal Biochem. 2012. PMID: 22342622
NSD2 is recruited through its PHD domain to oncogenic gene loci to drive multiple myeloma.
Huang Z, Wu H, Chuai S, Xu F, Yan F, Englund N, Wang Z, Zhang H, Fang M, Wang Y, Gu J, Zhang M, Yang T, Zhao K, Yu Y, Dai J, Yi W, Zhou S, Li Q, Wu J, Liu J, Wu X, Chan H, Lu C, Atadja P, Li E, Wang Y, Hu M. Huang Z, et al. Among authors: zhao k. Cancer Res. 2013 Oct 15;73(20):6277-88. doi: 10.1158/0008-5472.CAN-13-1000. Epub 2013 Aug 26. Cancer Res. 2013. PMID: 23980095
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. Kaniskan HÜ, et al. Among authors: zhao k. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27. Angew Chem Int Ed Engl. 2015. PMID: 25728001 Free PMC article.
Histone methyltransferase SETDB1 regulates liver cancer cell growth through methylation of p53.
Fei Q, Shang K, Zhang J, Chuai S, Kong D, Zhou T, Fu S, Liang Y, Li C, Chen Z, Zhao Y, Yu Z, Huang Z, Hu M, Ying H, Chen Z, Zhang Y, Xing F, Zhu J, Xu H, Zhao K, Lu C, Atadja P, Xiao ZX, Li E, Shou J. Fei Q, et al. Among authors: zhao k, zhao y. Nat Commun. 2015 Oct 16;6:8651. doi: 10.1038/ncomms9651. Nat Commun. 2015. PMID: 26471002 Free PMC article.
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
Lingel A, Sendzik M, Huang Y, Shultz MD, Cantwell J, Dillon MP, Fu X, Fuller J, Gabriel T, Gu J, Jiang X, Li L, Liang F, McKenna M, Qi W, Rao W, Sheng X, Shu W, Sutton J, Taft B, Wang L, Zeng J, Zhang H, Zhang M, Zhao K, Lindvall M, Bussiere DE. Lingel A, et al. Among authors: zhao k. J Med Chem. 2017 Jan 12;60(1):415-427. doi: 10.1021/acs.jmedchem.6b01473. Epub 2017 Jan 3. J Med Chem. 2017. PMID: 27992714
Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED.
Li L, Zhang H, Zhang M, Zhao M, Feng L, Luo X, Gao Z, Huang Y, Ardayfio O, Zhang JH, Lin Y, Fan H, Mi Y, Li G, Liu L, Feng L, Luo F, Teng L, Qi W, Ottl J, Lingel A, Bussiere DE, Yu Z, Atadja P, Lu C, Li E, Gu J, Zhao K. Li L, et al. Among authors: zhao k, zhao m. PLoS One. 2017 Jan 10;12(1):e0169855. doi: 10.1371/journal.pone.0169855. eCollection 2017. PLoS One. 2017. PMID: 28072869 Free PMC article.
7,217 results