HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)
- Name Andrew Riley ; Barry Potter
- Institute University of Bath
Tool name: HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)
Alternate names: HDACs; Histone deacetylases; SMRT; silencing mediator for retinoid or thyroid-hormone receptors; Nuclear receptor co-repressor 2; NCOR2; HDAC:SMRT3; 2-FAM-InsP5; T3 receptor-associating cofactor 1; TRAC-1
Molecular formula: C29H32NO27P5.4.5Et3N
Tool type: Small molecules
Description: Class I histone deacetylase (HDAC) enzymes are involved in epigenetic gene regulation by controlling acetylation of lysine sidechains in histone tails They form a catalytic subunit for other large protein complexes that repress gene expression when targeted to genomic DNA. The Class I HDAC family includes HDACs 1, 2, 3 & 8, however only HDAC3 is recruited exclusively to the SMRT co-repressor complex.
Functional and structural studies of HDACs when bound to their cognate corepressors has revealed that the regulation of their activity is controlled intracellularly by inositol phosphates. The molecule, Ins(1,4,5,6)P4, had been found to locate in the binding pocket formed between HDAC3 and SMRT.
The transcriptional coregulatory protein SMRT contains several nuclear receptor-interacting domains possessing modulatory functions including several autonomous repression domains. SMRT functions as a repressive coregulatory factor (corepressor) for many transcription factor pathways. SMRT also functions as a platform, facilitating the recruitment of histone deacetylases to the DNA promoters bound by its interacting transcription factors. Targeting HDACS provides promising epigenetic therapies for many diseases including Alzheimer's and spinal muscular atrophy.
Research area: Cancer ; Drug Discovery & Development ; Stem Cell Biology
- For Research Use Only
- • Watson et al. 2016. Nat Commun. 7:11262. PMID: 27109927.