Structural basis for KDM5A histone lysine demethylase inhibition by diverse compounds

The KDM5/JARID1 family of Fe(II)- and α-ketoglutarate-dependent demethylases removes methyl groups from methylated lysine 4 of histone H3. Accumulating evidence supports a role for KDM5 family members as oncogenic drivers. We compare the in vitro inhibitory properties and binding affinity of ten div...

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Pubblicato in:Cell Chem Biol
Autori principali: Horton, John R., Liu, Xu, Gale, Molly, Wu, Lizhen, Shanks, John R., Zhang, Xing, Webber, Philip J., Bell, Joshua S.K., Kales, Stephen C, Mott, Bryan T, Rai, Ganesha, Jansen, Daniel J, Henderson, Mark J, Urban, Daniel J, Hall, Matthew D, Simeonov, Anton, Maloney, David J, Johns, Margaret A., Fu, Haian, Jadhav, Ajit, Vertino, Paula M., Yan, Qin, Cheng, Xiaodong
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2016
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4958579/
https://ncbi.nlm.nih.gov/pubmed/27427228
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2016.06.006
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