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...

Ful tanımlama

Kaydedildi:
Detaylı Bibliyografya
Yayımlandı:Medchemcomm
Asıl Yazarlar: 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.
Materyal Türü: Artigo
Dil:Inglês
Baskı/Yayın Bilgisi: 2014
Konular:
Article
Online Erişim:https://ncbi.nlm.nih.gov/pmc/articles/PMC4678576/
https://ncbi.nlm.nih.gov/pubmed/26682034
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/C4MD00291A
Etiketler: Etiketle
Etiket eklenmemiş, İlk siz ekleyin!

Benzer Materyaller