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Sinefungin derivatives as inhibitors and structure probes of protein lysine methyltransferase SETD2Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gammaA chemical probe selectively inhibits G9a and GLP methyltransferase activity in cellsOpen access chemical probes for epigenetic targetsDiscovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9aSmall-Molecule Ligands of Methyl-Lysine Binding ProteinsStructure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic MutationsAn allosteric inhibitor of protein arginine methyltransferase 3Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9aDiscovery of a Potent Class I Protein Arginine Methyltransferase Fragment InhibitorPharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1Accessing protein methyltransferase and demethylase enzymology using microfluidic capillary electrophoresisChemical probes targeting epigenetic proteins: Applications beyond oncology.Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1Identification of novel functionally selective κ-opioid receptor scaffolds.The promise and peril of chemical probes.Structure-activity relationship studies of SETD8 inhibitors.Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors.Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolinesA potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.Identification of structure-activity relationships from screening a structurally compact DNA-encoded chemical library.Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain.Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.SET9-Mediated Regulation of TGF-β Signaling Links Protein Methylation to Pulmonary Fibrosis.Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.Epigenetic chemical probes.
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description
hulumtues
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researcher
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հետազոտող
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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পিটার জে ব্রাউন
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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Peter J Brown
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পিটার জে ব্রাউন
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P106
P21
P31
P496
0000-0002-8454-0367