A modified positron emission tomography (PET) imaging method enables real-time monitoring of epigenetic regulation of gene expression in the living human brain. The method uses a radioactively labeled, blood brain barrier-penetrant, small molecule called “Martinostat”, which binds histone deacetylases (HDACs), enzymes that regulate gene expression by modifying the chromatin acetylation state. According to the paper in the August 10 Science Translational Medicine, proof-of principle experiments in healthy individuals revealed a stereotypic pattern of HDAC expression in different brain regions. In order to investigate whether deviations from this pattern may occur in disease states, the investigators are now examining people with schizophrenia and Huntington’s disease. This approach could yield insights on epigenetic mechanisms in ALS and potential new therapeutic strategies, despite disappointments to date with HDAC inhibitors as ALS therapies (Piepers et al., 2009).
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Wey HY, Gilbert TM, Zürcher NR, She A, Bhanot A, Taillon BD, Schroeder FA, Wang C, Haggarty SJ, Hooker JM. Insights into neuroepigenetics through human histone deacetylase PET imaging. Sci Transl Med. 2016 Aug 10;8(351):351ra106. [Pubmed].