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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 |
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| Hlavní autoři: | , , , , , , , , , , , , , , , , , , , , , , |
| Médium: | Artigo |
| Jazyk: | Inglês |
| Vydáno: |
2018
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| Témata: | |
| 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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