Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

A potent inhibitor of the JmjC histone lysine demethylase KDM2A (compound 35, pIC(50) 7.2) with excellent selectivity over representatives from other KDM subfamilies has been developed; the discovery that a triazolopyridine compound binds to the active site of JmjC KDMs was followed by optimisation...

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Detalles Bibliográficos
Autores principales: England, Katherine S., Tumber, Anthony, Krojer, Tobias, Scozzafava, Giuseppe, Ng, Stanley S., Daniel, Michelle, Szykowska, Aleksandra, Che, KaHing, von Delft, Frank, Burgess-Brown, Nicola A., Kawamura, Akane, Schofield, Christopher J., Brennan, Paul E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4678576/
https://www.ncbi.nlm.nih.gov/pubmed/26682034
http://dx.doi.org/10.1039/C4MD00291A

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4678576/
https://www.ncbi.nlm.nih.gov/pubmed/26682034
http://dx.doi.org/10.1039/C4MD00291A

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