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EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature (2012) 7.01

SUZ12 is required for both the histone methyltransferase activity and the silencing function of the EED-EZH2 complex. Mol Cell (2004) 6.90

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Many paths to methyltransfer: a chronicle of convergence. Trends Biochem Sci (2003) 5.65

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Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas. Proc Natl Acad Sci U S A (2010) 4.52

Ezh1 and Ezh2 maintain repressive chromatin through different mechanisms. Mol Cell (2008) 4.44

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A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol (2012) 3.89

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Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov (2009) 3.50

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The Arabidopsis thaliana genome contains at least 29 active genes encoding SET domain proteins that can be assigned to four evolutionarily conserved classes. Nucleic Acids Res (2001) 2.70

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G9a and Glp methylate lysine 373 in the tumor suppressor p53. J Biol Chem (2010) 2.64

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Downregulation of histone H3 lysine 9 methyltransferase G9a induces centrosome disruption and chromosome instability in cancer cells. PLoS One (2008) 2.52

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol (2009) 2.50

EHMT1 controls brown adipose cell fate and thermogenesis through the PRDM16 complex. Nature (2013) 2.40

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Recognizing and exploiting differences between RNAi and small-molecule inhibitors. Nat Chem Biol (2007) 2.31

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood (2013) 2.28

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Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A (2013) 2.26

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EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis. Blood (2010) 2.11

Probing the probes: fitness factors for small molecule tools. Chem Biol (2010) 2.08

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett (2012) 2.04

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Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem (2009) 1.92

A role for repressive histone methylation in cocaine-induced vulnerability to stress. Neuron (2011) 1.92

An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol (2013) 1.89

DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis. Blood (2011) 1.88

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Subunit contributions to histone methyltransferase activities of fly and worm polycomb group complexes. Mol Cell Biol (2005) 1.78

Further clinical and molecular delineation of the 9q subtelomeric deletion syndrome supports a major contribution of EHMT1 haploinsufficiency to the core phenotype. J Med Genet (2009) 1.74

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem (2010) 1.73

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun (2012) 1.67

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Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem (2011) 1.46

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G9a/GLP-dependent histone H3K9me2 patterning during human hematopoietic stem cell lineage commitment. Genes Dev (2012) 1.40

Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens. J Biomol Screen (2012) 1.30

Deregulation of histone lysine methyltransferases contributes to oncogenic transformation of human bronchoepithelial cells. Cancer Cell Int (2008) 1.26

DOT1L regulates dystrophin expression and is critical for cardiac function. Genes Dev (2011) 1.25

The methyltransferase G9a regulates HoxA9-dependent transcription in AML. Genes Dev (2014) 1.23

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem (2013) 1.23

SET7/9 mediated methylation of non-histone proteins in mammalian cells. Epigenetics (2009) 1.16

Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L. Chem Biol Drug Des (2012) 1.12

EVI-1 interacts with histone methyltransferases SUV39H1 and G9a for transcriptional repression and bone marrow immortalization. Leukemia (2009) 1.10

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A (2014) 1.09

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A medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L. J Med Chem (2013) 0.95

Essential role of DOT1L in maintaining normal adult hematopoiesis. Cell Res (2011) 0.93

Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases. Q Rev Biophys (2013) 0.93

Small molecule control of chromatin remodeling. Chem Biol (2014) 0.88

Methyltransferase G9A regulates T cell differentiation during murine intestinal inflammation. J Clin Invest (2014) 0.86

Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer. Cell (2012) 3.77

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Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci U S A (2011) 1.98

Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem (2009) 1.92

An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol (2013) 1.89

Ultrafast permeation of water through protein-based membranes. Nat Nanotechnol (2009) 1.87

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Combined PI3K/mTOR and MEK inhibition provides broad antitumor activity in faithful murine cancer models. Clin Cancer Res (2012) 1.74

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem (2010) 1.73

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol (2013) 1.72

Accessing protein methyltransferase and demethylase enzymology using microfluidic capillary electrophoresis. Chem Biol (2010) 1.67

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Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem (2011) 1.46

Small-molecule ligands of methyl-lysine binding proteins. J Med Chem (2011) 1.45

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The methyltransferase G9a regulates HoxA9-dependent transcription in AML. Genes Dev (2014) 1.23

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem (2013) 1.23

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Targets in epigenetics: inhibiting the methyl writers of the histone code. Curr Chem Genomics (2011) 1.03

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Selective inhibitors of protein methyltransferases. J Med Chem (2014) 1.01

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Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors. J Med Chem (2013) 1.00

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Efficient visible-light photocatalytic hydrogen evolution and enhanced photostability of core/shell CdS/g-C3N4 nanowires. ACS Appl Mater Interfaces (2013) 0.93

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Writing and rewriting the epigenetic code of cancer cells: from engineered proteins to small molecules. Mol Pharmacol (2012) 0.88

Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem (2013) 0.88

Automated iterative MS/MS acquisition: a tool for improving efficiency of protein identification using a LC-MALDI MS workflow. Anal Chem (2011) 0.88

A "tagless" strategy for identification of stable protein complexes genome-wide by multidimensional orthogonal chromatographic separation and iTRAQ reagent tracking. J Proteome Res (2008) 0.88

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Phase transformation guided single-layer β-Co(OH)₂ nanosheets for pseudocapacitive electrodes. ACS Nano (2014) 0.82

Photothermal-Responsive Single-Walled Carbon Nanotube-Based Ultrathin Membranes for On/Off Switchable Separation of Oil-in-Water Nanoemulsions. ACS Nano (2015) 0.82

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Layer-by-layer engineered Co-Al hydroxide nanosheets/graphene multilayer films as flexible electrode for supercapacitor. Langmuir (2011) 0.81

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Expression, purification, and characterization of recombinant human serum albumin fusion protein with two human glucagon-like peptide-1 mutants in Pichia pastoris. Protein Expr Purif (2008) 0.80

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Dual-label time-resolved fluoroimmunoassay for simultaneous detection of aflatoxin B1 and ochratoxin A. Arch Toxicol (2009) 0.80

Free-standing single-walled carbon nanotube-CdSe quantum dots hybrid ultrathin films for flexible optoelectronic conversion devices. Nanoscale (2012) 0.80

A one-step automated high-radiochemical-yield synthesis of 18F-FECNT from mesylate precursor. Appl Radiat Isot (2008) 0.80

EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells. Cancer Biol Ther (2014) 0.80

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Absence of Yps7p, a putative glycosylphosphatidylinositol-linked aspartyl protease in Pichia pastoris, results in aberrant cell wall composition and increased osmotic stress resistance. FEMS Yeast Res (2012) 0.79

Total flavonoids of Flos Chrysanthemi protect arterial endothelial cells against oxidative stress. J Ethnopharmacol (2011) 0.79