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Discovery of a Highly Selective Cell‐Active Inhibitor of the Histone Lysine Demethylases KDM2/7

Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell‐permeable inhibitors or suitable tool compounds for these enzymes. We describe the discovery of a new class of inhibitor that is highly potent towards the...

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Detalhes bibliográficos
Publicado no:Angew Chem Int Ed Engl
Principais autores: Gerken, Philip A., Wolstenhulme, Jamie R., Tumber, Anthony, Hatch, Stephanie B., Zhang, Yijia, Müller, Susanne, Chandler, Shane A., Mair, Barbara, Li, Fengling, Nijman, Sebastian M. B., Konietzny, Rebecca, Szommer, Tamas, Yapp, Clarence, Fedorov, Oleg, Benesch, Justin L. P., Vedadi, Masoud, Kessler, Benedikt M., Kawamura, Akane, Brennan, Paul E., Smith, Martin D.
Formato: Artigo
Idioma:Inglês
Publicado em: John Wiley and Sons Inc. 2017
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5725665/
https://ncbi.nlm.nih.gov/pubmed/28976073
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.201706788
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