In the case of the HDAC assays, there were three targets,
HDAC1, HDAC3 and HDAC6, tested with 41, 2 and 3 reference chemicals, respectively.
Mocetinostat (MGCD0103) is an isotype of HDACI and showed in vitro activity against
HDAC1 selectively and some activity against the various isoforms of HDAC (2, 3, and 11).
After cells were grown to 30-50% confluence, 80 nmol/L small interfering RNA (siRNA) specific for
Hdac1 (siG1379144052, GuangZhou RiboBio.
MeCP2 has also its role in anchoring a multiprotein repressory complex to the DNA which is responsible for deacetylation of histones and alterations of chromatin by recruiting deactylases
HDAC1 and HDAC2 also shown in Fig.
Interestingly,
HDAC1 has been reported to be overexpressed in HCC; yet, HDAC6 has been found to be decreased in HCCs compared with adjacent control tissues, and this observation is associated with poor prognosis (104).
Both HAT and HDAC enzymes, such as GCN5/KAT2A and
HDAC1, respectively, are subunits in multiprotein complexes (Grant et al.
Similarly, in pituitary tumourigenesis, HMGA2 displaces
HDAC1 from the complex Rb/E2F1, leaving the latter in an active acetylated form [81].
Hu et al., "
HDAC1 knockdown inhibits invasion and induces apoptosis in non-small cell lung cancer cells," Biological Chemistry, vol.
[70] which demonstrated that a low level of chronic oxidative stress results in the malignant transformation of human renal tubular epithelial cells, and the potential role is the aberrant expression of epigenetic regulatory genes involved in DNA methylation (DNMTs) as well as histone modifications (
HDAC1, HAT1) in human renal tubular epithelial cells malignantly transformed by chronic oxidative stress.
The authors reported that
HDAC1 and HDAC2 were downregulated, which are associated with an increase in H3K4me3 and H3K9Ac and which are associated with an active chromatin state [7].
Su et al., "Interaction of FUS and
HDAC1 regulates DNA damage response and repair in neurons," Nature Neuroscience, vol.
Cano, "Snail mediates E-cadherin repression by the recruitment of the Sin3A/histone deacetylase 1 (
HDAC1)/HDAC2 complex," Molecular and Cellular Biology, vol.