C05053: Small Molecules Epigenetic Inhibitors for Cancer Prevention and Treatment.
Value Proposition: • Compounds represent first in class small molecule agents for inhibition of MBD2 activity. • Reversible inhibition. • Truly epigenetic agents, unlike other epigenetic drugs which appear to have cytotoxic effects independent of epigenetic mechanisms (e.g. DNMT inhibitors and HDAC inhibitors). • Results showing efficacy of lead compounds alone and in rational combinatorial strategies in cancer models are also available.
Technical Details:
JHU scientists have identified small molecules inhibitors of the transcriptional repression pathway mediated by the 5m-CpG-binding family domain proteins (MBD), MBD2 and MeCP2. Both MBD2 and MeCP2 have been found to play critical roles in both the epigenetic silencing of gene in human cancer cells and in the development of intestinal adenomas in APC min/+ mice. The inhibitors describes in this invention can be used to reverse the epigenetic silencing of critical genes that accompanies cancer development
Looking for Partners:
The inhibitors can be developed for the treatment of multiple cancers and sickle cell anemia.
Publications: Issued US Patent 9,034,574
