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Site-specific histone modification and DNA methylation
directly and indirectly impact transcriptional regulation
and the direction of other cellular processes. The biological
influences achieved by various histone and DNA modifying
enzymes eventually require that histone and DNA be modified.
Epigenetic modifications can be modulated by directly
inhibiting modifying enzymes or blocking co-factor recruiting
pathways. Development of these modulators would lead to
the development of new therapeutic agents and improvement
in disease treatment, especially cancer therapy. The EpiModifer™
screening system provides a platform that allows
the screening of modulators that target site-specific
histone modifications, global DNA methylation, and functional
region-specific DNA methylation.
Current Panel of EpiModifier™ Targets:
| Histone Acetylation |
Histone Methylation |
Histone Phosphorylation |
DNA Methylation |
| H3-k9 |
H3-K4 |
H2AX |
Global Methylation |
| H3-k14 |
H3-K9 |
H2B |
Tumor Suppression Panel |
| H3-k18 |
H3-K14 |
H3 (Ser10) |
Oncogene Panel |
| H3-k23 |
H3-K27 |
H3 (Ser28) |
Drug Resistance Panel |
| H3-k27 |
H3-K36 |
H3 (Thr11) |
Apoptosis Panel |
| H4-k5 |
H3-R2 |
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Cell Cycle Panel |
| H4-k8 |
H3-R17 |
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DNA Damage Repair Panel |
| H4-k9 |
H4-R3 |
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Angiogenesis Panel |
| H4-k12 |
Histone H3 |
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Metastasis Panel |
| H4-k16 |
Histone H4 |
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Nuclear Receptor Panel |
| Histone H3 |
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Cytokine Panel |
| Histone H4 |
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Transcription Factor Panel |
| Histone H2A |
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Assay Principles
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See also:
Epigenase™ Epigenetic Enzyme Inhibitor Screening
System
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