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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Bibliografiset tiedot
Julkaisussa:J Med Chem
Päätekijät: 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
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: 2018
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Article
Linkit: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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