A chemoprobe tracks its target [Methods and Resources]
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. MascarĂ³ et al. describe a luminescence-based ELISA approach that directly monitors binding of inhibitors to the histone lysine demethylase KDM1A.
Source: Journal of Biological Chemistry - Category: Chemistry Authors: Aseem Z. Ansari Tags: Editors ' Picks Highlights Source Type: research