Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders. The first KDM inhibitors for KDM1 have entered clinical trials, and efforts are ongoing to develop potent, selective and cell-active ‘probe’ molecules for this target class. Robust cellular assays to assess the specific engagement of KDM inhibitors in cells as well as their c...
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- Peer reviewed
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- (FP7/2007-2013) Innovative Medicines Initiative Joint Undertaking under Grant Agreement No. 115766
- BioMed Central Publisher's website
- Epigenetics and Chromatin Journal website
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- Hatch et al.
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- © The Author(s) 2017. Open Access: This article is distributed under the terms of the Creative Commons Attribution 4.0 International License.
Assessing histone demethylase inhibitors in cells: lessons learned
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