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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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5725665/
https://www.ncbi.nlm.nih.gov/pubmed/28976073
http://dx.doi.org/10.1002/anie.201706788