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Proceedings of the National Academy of Sciences - PNAS, ISSN 0027-8424, 9/2014, Volume 111, Issue 35, pp. 12853 - 12858
.... Here, we report the discovery of (R)-PFI-2—a first-in-class, potent ($K_i^{app}$ = 0.33 nM), selective, and cell-active inhibitor of the methyltransferase activity of human SETD7... 
Enzymes | Transcriptional regulatory elements | Genes | Cell lines | Histones | Gene expression regulation | Kinetics | Methylation | Inhibitory concentration 50 | Chemicals | Chemical biology | Epigenetics | Chemical probe | Science & Technology - Other Topics | Multidisciplinary Sciences | Science & Technology | Humans | Methyltransferases - metabolism | Structure-Activity Relationship | Phosphoproteins - metabolism | Pyrrolidines - pharmacology | Dose-Response Relationship, Drug | Histone-Lysine N-Methyltransferase - antagonists & inhibitors | MCF-7 Cells | Tetrahydroisoquinolines - chemistry | Enzyme Inhibitors - chemistry | Epigenesis, Genetic - drug effects | Protein Structure, Tertiary | Tetrahydroisoquinolines - pharmacology | Histone-Lysine N-Methyltransferase - genetics | Sulfonamides - chemistry | Enzyme Inhibitors - pharmacology | Protein-Serine-Threonine Kinases - genetics | Phosphoproteins - genetics | Sulfonamides - pharmacology | Pyrrolidines - chemistry | Methyltransferases - antagonists & inhibitors | Histone-Lysine N-Methyltransferase - metabolism | Signal Transduction - drug effects | Fibroblasts - drug effects | Adaptor Proteins, Signal Transducing - genetics | Mutation | Adaptor Proteins, Signal Transducing - metabolism | Protein research | Research | Methyltransferases | Lysine | Health aspects | Protein-protein interactions | chemical probe | Biological Sciences | chemical biology | epigenetics
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Nature Immunology, ISSN 1529-2908, 01/2011, Volume 12, Issue 1, pp. 29 - 36
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Proceedings of the National Academy of Sciences - PNAS, ISSN 1091-6490, 12/2008, Volume 105, Issue 49, pp. 19229 - 19234
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Nature (London), ISSN 1476-4687, 02/2016, Volume 530, Issue 7591, pp. 447 - 452
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Nature (London), ISSN 1476-4687, 2010, Volume 464, Issue 7290, pp. 927 - 931
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