Host: The Japanese Pharmacological Society
Name : The 97th Annual Meeting of the Japanese Pharmacological Society
Number : 97
Location : [in Japanese]
Date : December 14, 2023 - December 16, 2023
Histone post-translational modification is one of important epigenetic mechanisms to regulate chromatin structures and gene expression. Many kinds of histone-modifying enzymes are reported, and regulation strategies for such protein complexes have been actively studied. In the field of chemical epigenetics, it is highly demanded to develop novel molecules that can modulate activity of target histone-modifying enzymes. However, it is still difficult to identify specific modulators due to the structural complexity of these types of proteins.
We aimed to develop novel molecules that modulate the levels of histone H3 lysine 27 (H3K27) methyl marks by targeting polycomb repressive complex 2 (PRC2). PRC2 contains four subunits (EZH2, EED, SUZ12 and RbAp46/48), and catalyzes sequential methylation reactions at H3K27. Both the gain-of-function and loss-of-function mutations of PRC2 have been reported in several types of cancers. Therefore, development of PRC2 inhibitors, and also activators can be effective for some types of cancers.
In the presentation, our recent results will be shown to discuss strategies for modulation of H3K27 methylation with molecules.
