Analytical Sciences

Chemical Tools for Probing Histone Deacetylase (HDAC) Activity

Masafumi MINOSHIMA*,** and Kazuya KIKUCHI*,***

*Graduate School of Engineering, Osaka University, 2-1 Yamadaoka, Suita, Osaka 565-0871, Japan
**Institute of Academic Initiatives, Osaka University, 2-1 Yamadaoka, Suita, Osaka 565-0871, Japan
***Immunology Frontier Research Center (IFReC), Osaka University, 2-1 Yamadaoka, Suita, Osaka 565-0871, Japan

Histone deacetylases (HDACs) enzymes are responsible for removing epigenetic markers on histone proteins, which results in chromatin inactivation and gene repression. An evaluation of HDAC activity is essential for not only determining the physiological function of HDACs, but also for developing HDAC-targeting drugs. This review focuses on the chemical tools used to detect HDAC activity. We highlight activity-based probes and positron emission tomography probes based on the chemical structure of the inhibitors. We also summarize fluorogenic probes used in single-step methods for HDAC detection. These fluorogenic probes are designed based on the nucleophilicity of the amino group, aggregation via electrostatic interactions, and changes in the DNA binding properties. These fluorogenic systems may enable facile and rapid screening to evaluate HDAC inhibitors, which will contribute to the development of epigenetic drugs.

J-STAGE: View this article in J-STAGE