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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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Bibliographic Details
Published in:Cell Chem Biol
Main Authors: 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
Format: Artigo
Language:Inglês
Published: 2016
Subjects:
Online Access: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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