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The enzymes included in the Epigenase™
screening system are with important biological and therapeutic
relevance. Misregulation of these enzymes may lead to
disease state such as cancer. Inhibitors that target to
these enzymes such as HDACs and Dnmts have proven effective
as novel cancer therapeutic agents. It has been found
that different form of HDACs or Dnmts may play distinct
role in biological processes. Thus the continued development
of these inhibitors, especially isoform-selective inhibitors,
would further improve cancer treatment. With a proprietary
technology, the Epigenase™ screening system provides
a platform that not only allows the testing of inhibitors
against total enzymatic activity but also allows the screening
of inhibitors specific to individual HDACs and Dnmts.
Current Panel of Epigenase™ Targets:
| Histone Deacetylase (HDACs) |
Histone Methyltransferase (HMTs) |
DNA Methyltransferase (Dnmts) |
| Total HDACs |
G9a |
Total Dnmts |
| HDAC-1 |
SET7/9 |
Dnmt1 |
| HDAC-2 |
ASH1 |
Dnmt3A |
| HDAC-3 |
ALL-1 |
Dnmt3B |
| HDAC-4 |
MLL |
|
| HDAC-5 |
SMYD3 |
|
| HDAC-6 |
SUV39H1 |
|
| HDAC-7 |
SUV39H2 |
|
| HDAC-8 |
SETDB1 |
|
| HDAC-9 |
NSD1 |
|
| HDAC-10 |
DOT1 |
|
| HDAC-11 |
EZH2 |
|
| SIRT-1 |
PRMT1 |
|
| SIRT-2 |
PRMT4 |
|
| SIRT-3 |
|
|
| SIRT-4 |
|
|
| SIRT-5 |
|
|
| SIRT-6 |
|
|
| SIRT-7 |
|
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Assay Principles
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See also:
EpiModifer™
Epigenetic Modulator Screening System
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