Although it may sound like the name of a DJ in a Vegas nightclub, DZNep is actually a histone methylation inhibitor, and has recently created some buzz when it was found to inhibit H3K27 and H4K20 methylation and reactivate silenced genes in cancer cells. Sensing the therapeutic possibilities, Peter Jones and his team at USC decided to look into DZNep to see how it works. Here are some of the things they found:
- DZNep is actually a global histone methylation inhibitor, acting on both repressive and active histone marks, not just H3K27 and H4K20 as previously thought.
- Repressive histone marks can be reversed by DZNep, but transcripts can’t be re-expressed if it has a methylated CpG island.
- The somatic changes induced by DZNep were not heritable, and would return once the drug was withdrawn.
- Although DZNep might not be destined to become a cancer drug on its own, it’s a valuable research tool, targeting multiple histone marks at once.
- Combination cancer therapies using DZNep and 5-Aza-CdR (or others) could prove effective by targeting different epigenetic pathways at once (histone methylation and DNA Methylation).
For all the nitty-gritty info and details, head over to Molecular Cancer Therapeutics, June 2009