Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A

The active sites of hundreds of human α-ketoglutarate (αKG) and Fe(II)-dependent dioxygenases are exceedingly well preserved, which challenges the design of selective inhibitors. We identified a noncatalytic cysteine (Cys481 in KDM5A) near the active sites of KDM5 histone H3 lysine 4 demethylases, w...

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Publicado en:J Med Chem
Main Authors: Horton, John R., Woodcock, Clayton B., Chen, Qin, Liu, Xu, Zhang, Xing, Shanks, John, Rai, Ganesha, Mott, Bryan T., Jansen, Daniel J., Kales, Stephen C., Henderson, Mark J., Cyr, Matthew, Pohida, Katherine, Hu, Xin, Shah, Pranav, Xu, Xin, Jadhav, Ajit, Maloney, David J., Hall, Matthew D., Simeonov, Anton, Fu, Haian, Vertino, Paula M., Cheng, Xiaodong
Formato: Artigo
Idioma:Inglês
Publicado: 2018
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC6467790/
https://ncbi.nlm.nih.gov/pubmed/30392349
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01219
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