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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Bibliografske podrobnosti
izdano v: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
Format: Artigo
Jezik:Inglês
Izdano: 2018
Teme:
Article
Online dostop: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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