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RSS FeedsA chemoprobe tracks its target [Methods and Resources] (Journal of Biological Chemistry)

 
 

17 may 2019 10:01:42

 
A chemoprobe tracks its target [Methods and Resources] (Journal of Biological Chemistry)
 




Small-molecule inhibitors of histone-modifying enzymes have significant clinical utility for managing diseases such as cancer. These inhibitors are usually identified and monitored through their effects on the gain or loss of specific histone marks. In cells, multiple related enzymes can place or remove a specific mark; therefore, relying on an indirect measure of inhibitor engagement can be misleading. Mascaró et al. describe a luminescence-based ELISA approach that directly monitors binding of inhibitors to the histone lysine demethylase KDM1A.


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43 viewsCategory: Biochemistry
 
Chemoprobe-based assays of histone lysine demethylase 1A target occupation enable in vivo pharmacokinetics and pharmacodynamics studies of KDM1A inhibitors [Genomics and Proteomics] (Journal of Biological Chemistry)
Structural and mechanistic basis of mammalian Nudt12 RNA deNADding (Nature Chemical Biology)
 
 
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