Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
Nathan R Rose, Stanley S Ng, Jasmin Mecinović, Benoît M R Liénard, Simon H Bello, Zhe Sun, Michael A McDonough, Udo Oppermann, Christopher J Schofield
文献索引:J. Med. Chem. 51 , 7053-6, (2008)
全文:HTML全文
摘要
The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.
相关化合物
相关文献:
2015-10-01
[Cell Death Differ. 22 , 1618-29, (2015)]
2015-01-01
[J. Neuroinflammation 12 , 110, (2015)]
1994-06-01
[Clin. Chem. 40(6) , 862-6, (1994)]
2007-05-01
[Nat. Chem. Biol. 3(5) , 268-273, (2007)]
2009-02-12
[Nature 457(7231) , 910-4, (2009)]