EC Number |
Activating Compound |
Reference |
---|
1.14.11.69 | ascorbate |
- |
744722 |
1.14.11.69 | ascorbate |
required |
700209, 753157 |
1.14.11.69 | fisetin |
fisetin induces DNA damage via critical transcription factor RFXAP/KDM4A-dependent histone H3K36 demethylation, thus causing inhibition of proliferation in pancreatic adenocarcinoma (PDAC). Fisetin inhibits cell proliferation and induces DNA damage and S-phase arrest in PDAC. Expression of RFXAP and other DNA-damage response genes is upregulated by fisetin. RFXAP targets KDM4A. Overexpression of RFXAP upregulates KDM4A and attenuates methylation of H3K36, impairing DNA repair and enhancing the DNA damage induced by fisetin |
764436 |
1.14.11.69 | heterochromatin protein 1 |
predominant localization to centric heterochromatin. HP1a, when resident near centromeres, plays a role in the gene silencing associated with heterochromatin packaging. HP1a binding, two molecules HP1a per enzyme molecule, stimulates demethylation of H3K36me2 and H3K36me3 by dKDM4a, mechanism, overview. HP1a mutant V26M is inactive |
700202 |
1.14.11.69 | HP1 a protein |
HP1a, encoded by the Su(var)2-5 gene and involved in the establishment and maintenance of higher-order structure of heterochromatin, stimulates the histone H3K36 demethylation activity of dKDM4A, and this stimulation depends on the H3K9me-binding motif of HP1a. HP1a and dKDM4A interact with each other, and loss of HP1a leads to an increased level of histone H3K36me3. The CSD of HP1a and a consensus HP1-interacting PxVxL motif in dKDM4A are responsible for the HP1a-dKDM4A interaction |
700209 |
1.14.11.69 | HP1a |
HP1a targets the H3K36 demethylase dKDM4A to heterochromatic genes, it is required for dKDM4A-mediated H3K36me3 demethylation at a subset of heterochromatic genes. Demethylation activity of dKDM4A at euchromatin is independent of HP1a targeting |
726301 |