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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Vydáno v:J Med Chem
Hlavní autoři: 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
Médium: Artigo
Jazyk:Inglês
Vydáno: 2018
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Article
On-line přístup: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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