Study enzyme kinetics, and screen small molecular inhibitors of JMJ for drug discovery and HTS applications.
Biochem/physiol Actions
Histone proteins are basic building blocks of chromatin. Post-translational modifications of histone tails controls chromatin organization and gene transcription. Histone H3 lysine 9 dimethylation (H3K9me2) serves as an epigenetic marker for gene repression and silencing. This modification plays a significant role in embryogenesis and carcinogenesis. Histone methyltransferase G9a is responsible for hypoxic stress-mediated H3K9me2 in mammalian cells
General description
The mammalian chromatin is present in nucleosomes, made of histone octamers (H2A,H2B,H3,H4)2. Mammals contain three main classes of histone H3 variants: the replicative histones (H3.1 and H3.2), the replacement histone (H3.3) and the centromeric histone (Cenp-A). Dimethylated histone H3 lysine 9 (H3K9me2) is mainly present in euchromatin and is linked with repressed promoter areas.