Nucleosomes are basis units of DNA packaging in eukaryotic cells. A core particle (mono-nucleosome) consists of a segment of DNA called core DNA (147 bp in length) wound around a histone octamer (Fig 1.). Histone octamers are made up of 2 copies of the the core histones H2A, H2B, H3, and H4. These mono-nucleosomes are connected by linker 80bp-long DNA. H1 histone, the so-called linker histone, binds to the linker DNA close to the entry and exit of the core DNA and is involved in chromatin compaction (Fig 1.). [Read more…]
Histone Methyltransferases (ex. EZH1 and EZH2, and G9a) and their counter-parts (Histone demethylases like JARID1, the KDM4, and the JMJD family) have become promising targets for inhibitor screenings, especially in Cancer drug discovery. (1, 2) Accessing a wide variety of pure and well-characterized bioactive small molecules is of importance when characterizing these enzymes.
Here, we’ve compiled a list of 19 bioactive compounds currently seen in the literature when studying Histone Methyltransferases and Demethylases in Drug Discovery. [Read more…]